Selleck.Co.Uk: Inhibitors, Antibodies, Proteins, Kits and Reagents

BRM/BRG1 ATP Inhibitor-1 (BRM014)

BRM/BRG1 ATP Inhibitor-1 (Compound 14) is an orally active inhibitor of Brahma Homolog (BRM)/SMARCA2 (BRG1) with IC50s below 0.005 µM.

PF-9363 (CTx-648)

PF-9363 is a potent and selective KAT6A/6B inhibitor with Ki of 0.41 nM and 1.2 nM for KAT6A and KAT6B, respectively. PF-9363 displays potent anti-tumour activity in ER+ breast cancer models.

Setmelanotide (RM-493)

Setmelanotide (RM-493, BIM-22493, CAM 4072) is a cyclic peptide full agonist of melanocortin-4 receptor (MC4R) with an EC50 of 0.27 nM and a Ki of 2.1 nM.

SY-5609

SY-5609 (CDK7-IN-3) is an orally active and highly selective inhibitor of CDK7 with a KD value of 0.065 nM. SY-5609 exhibits poor inhibition on CDK2, CDK9, CDK12. SY-5609 displays antitumor activity and can induce apoptosis in tumour cells.

MRTX1133

MRTX1133 is a highly selective inhibitor of mutant KRAS G12D and can reversibly bind to the activated and inactivated KRAS G12D mutants and inhibit their activity. The specificity of MRTX1133 to KRAS G12D is more than 1000 times that of wild-type KRAS.

Lartesertib (M4076)

Lartesertib (M4076) inhibits Ataxia telangiectasia-mutated (ATM) kinase activity with a sub-nanomolar potency and shows remarkable selectivity against other protein kinases, suppresses DSB repair, clonogenic cancer cell growth, and potentiates antitumor activity of ionizing radiation in cancer cell lines.

TRULI (Lats-IN-1)

TRULI inhibits both Lats1 and Lats2 with an IC50 of 0.2 nM, suppresses YAP phosphorylation, induces cell proliferation in several cell lines and tissues, and promotes the initial stages of proliferative regeneration of the sensory receptors in the inner ear.

Nab-Paclitaxel

Nab-Paclitaxel is a novel solvent-free paclitaxel in which the binding ratio of paclitaxel to human albumin is approximately 1:9. It is an anti-microtubule drug that promotes microtubule aggregation in tubulin dimers and inhibits microtubule depolymerization to stabilise the microtubule system. Solutions are unstable and should be fresh-prepared.

Relacorilant (CORT125134)

Relacorilant (CORT125134) is a potent, selective and orally bioavailable Glucocorticoid Receptor antagonist, with a Ki of 7.2 nM in HepG2 TAT assay, and also shows Kis of 12, 81.2, 210 nM for rat, human and monkey Glucocorticoid Receptor in cell-based assay, respectively.

AU-15330

AU-15330 is a proteolysis-targeting chimera (PROTAC) degrader of the SWI/SNF ATPase subunits, SMARCA2 and SMARCA4, which can induce potent inhibition of tumour growth in xenograft models of prostate cancer.

Camonsertib (RP-3500)

Camonsertib (RP-3500) is a highly potent and selective inhibitor of ATR kinase with an IC50 of 1 nM.

BzATP triethylammonium salt

BzATP triethylammonium salt acts as a P2X receptor agonist with pEC50s of 8.74, 5.26, 7.10, 7.50, 6.19, 6.31, 5.33 for P2X1, P2X2, P2X3, P2X2/3, P2X4 and P2X7, respectively, also is potent at P2X7 receptors with EC50s of 3.6 μM and 285 μM for rat P2X7 and mouse P2X7, respectively.

Sirpiglenastat (DRP-104)

Sirpiglenastat (DRP-104) is a broad acting glutamine antagonist. It has anticancer effects by directly targeting tumour metabolism and simultaneously inducing a potent anti-tumour immune response with immunomodulatory and antineoplastic activities.

Osunprotafib (ABBV-CLS-484)

Osunprotafib (ABBV-CLS-484) is a potent PTPN1 or PTPN2 inhibitor with a sub-nanomolar activity.

Ziftomenib (KO-539)

Ziftomenib (KO-539) is an oral inhibitor of menin targeting the menin–KMT2A protein-protein interaction. It exhibits antileukemic activity and induces apoptosis of acute myeloid leukaemia (AML) cells.

TDI-011536

TDI-011536 is a potent Lats kinase inhibitor that interrupts Hippo-Yap signalling and promotes proliferation of lesioned cardiac muscle cells.

TNG908 (Ralometostat)

Ralometostat (TNG908) is a potent, selective, and brain-penetrant inhibitor of PRMT5 with an IC50 of 4 μM, acting through an MTA-cooperative mechanism. It also shows antitumor activity in a xenograft model.

IAG933

IAG933 (YAP-TEAD-IN-3) is a small molecule and acts as a YAP/TAZ-TEAD inhibitor. It also inhibits NCI-H2052 and can be used in research of tumour invasion and metastatic spread of solid tumours.

Brigimadlin

Brigimadlin (BI 907828) is a potent, orally active inhibitor of E3 ubiquitin-protein ligase MDM-2. Brigimadlin inhibits MDM-2's suppression of the tumour suppressor p53. It promotes Apoptosis and enhances the transcription of p53 targets such as p21 and PUMA in BT48, BT67, and BT73 cells.

PF-07220060 (CDK4/6-IN-6)

PF-07220060 (CDK4/6-IN-6) is a potent CDK4/CDK6 inhibitor with a Ki of 0.6 nM and 13.9 nM for CDK4/Cyclin D1 and CDK6/Cyclin D3, respectively.

Tulmimetostat (CPI-0209)

Tulmimetostat (CPI-0209) is an orally bioavailable and selective inhibitor of EZH2 that has therapeutic potential for androgen receptor-dependent prostate cancer.

ZEN-3694 (BET-IN-19)

ZEN-3694 is an orally bioavailable bromodomain extraterminal inhibitor (BETi) that leads to down-regulation of expression of AR-signalling in metastatic castration-resistant prostate cancer (mCRPC) models.

GNE-7883

GNE-7883 is a potent and allosteric small-molecule inhibitor of pan-TEAD, that allosterically blocks the interactions between YAP/TAZ and all human TEAD paralogs through binding to the TEAD lipid pocket. It effectively reduces chromatin accessibility at TEAD motifs, suppresses cell proliferation in a variety of cell line models and achieves strong antitumor efficacy in vivo. Furthermore, it effectively overcomes KRAS G12C inhibitor resistance.

Luxdegalutamide (ARV-766)

Luxdegalutamide (ARV-766) is an orally active and potent degrader of proteolysis targeting chimera (PROTAC) protein. ARV-766 degrades wild-type androgen receptor (AR) but also relevant AR LBD mutants, including the most prevalent AR L702H, H875Y, and T878A mutations.

Daraxonrasib (RMC-6236)

Daraxonrasib (RMC-6236) is a RAS(ON) multi-selective non-covalent inhibitor of the active, GTP-bound state of both mutant and wild-type variants of canonical RAS isoforms with broad therapeutic potential. RMC-6236 exhibits strong anticancer efficacy in RAS-addicted Cell Cycle lines, especially those with mutations at codon 12 of K-Ras.

Fluorofurimazine (FFz)

Fluorofurimazine (FFz) is a novel furimazine analogue, with increased aqueous solubility enabling higher signal emission than furimazine for bioluminescence imaging. Fluorofurimazine (FFz) enables higher substrate loading and improved optical imaging sensitivity in in-vivo.

Exarafenib (KIN-2787)

Exarafenib (KIN-002787, KIN-2787, RAF/KIN_2787) is an orally-available, selective inhibitor of pan-RAF. Exarafenib is effective in RAF-dependent cancers, including all classes of BRAF alterations. Exarafenib suppresses MAPK signalling in RAF-dependent melanoma cell lines. KIN-2787 exhibits low nanomolar to picomolar potency against RAF1, BRAF, and ARAF with an IC50 of 0.06-3.46 nM with minimal activity towards non-RAF kinases.

Vanzacaftor (VX-121)

Vanzacaftor (VX-121) is an orally active corrector of Cystic fibrosis transmembrane conductance regulator (CFTR). Vanzacaftor improves the processing and trafficking of CFTR protein and increases chloride transport in combination with Tezacaftor and Deutivacaftor.

Solutol HS-15 (Polyethylene glycol 12-hydroxystearate)

Solutol HS-15 (Polyethylene glycol 12-hydroxystearate) is a Macrogol 15 hydroxy stearate, which improves permeability by disrupting the membrane structure/fluidity change. Note: Due to its chemical properties, this product will be semi-solid and solid at room temperature and low temperature.

STC-15

STC-15 is an oral, small-molecule inhibitor of RNA methyltransferase METTL3. It inhibits tumour growth through the activation of anti-cancer immune responses associated with increased interferon signalling and synergises with T-cell checkpoint blockade.

Deutivacaftor (VX-561, Ivacaftor-D9)

VX-561 (CTP-656) is a potent CFTR modulator and exhibits an EC50 value of 255 nM for CFTR potentiation in G551D/F508del HBE cells.

Tersolisib (STX-478)

Tersolisib (STX-478) is a highly potent, mutant-selective, allosteric inhibitor of PI3Kα, that selectively targets prevalent mutant forms of PI3Kα. It demonstrates strong efficacy against common PI3Kα helical- and kinase-domain mutations, including the H1047R variant, with an IC50 value of 9.4 nmol/L. STX-478 exhibits 14-fold greater selectivity for mutant PI3Kα over the wild-type form. It spares metabolic dysfunction and improves therapeutic response in PI3Kα-Mutant Xenografts.

INX-315

INX-315 is an orally active and selective inhibitor of CDK2 that induces Cell Cycle arrest in the G1 phase. It exhibits an IC50 value of 2.3 nM in intracellular NanoBRET assay, respectively. It displays a 50-fold increased CDK2 selectivity compared to CDK1. INX-315 decreases the phosphorylation of CDK2 substrates and suppresses tumor growth in xenograft mouse models in a dose-dependent manner.

RMC-7977

RMC-7977 is a potent, reversible, tri-complex oral inhibitor that selectively targets active (GTP-bound) forms of KRAS, HRAS, and NRAS, which exhibits broad-spectrum activity against both mutant and wild-type variants (a RAS^MULTI (ON) inhibitor). It also exhibits significant anti-tumour efficacy in pancreatic ductal adenocarcinoma (PDAC).

HRO761

HRO761 is a potent, selective, allosteric inhibitor of Werner syndrome RecQ helicase (WRN). It binds at the interface of the D1 and D2 helicase domains, locking WRN in an inactive conformation, and demonstrates anti-proliferative effects specifically in microsatellite instability (MSI) cancer cells.

NRL-1049

NRL-1049 (BA 1049) is a small molecule selective inhibitor of ROCK2 with an IC50 of 0.59 µM. It exhibits potent efficacy in preserving the blood-brain barrier (BBB) and suppresses seizures after brain injury, and inhibits haemorrhagic transformation after ischaemic stroke in mice.

ART899

ART899, a derivative of ART558 is a potent, specific allosteric inhibitor of DNA polymerase theta (Polθ), specifically inhibits Polθ MMEJ activity with IC50 of 180 nM. It specifically radiosensitizes tumour cells and have a potent stand-alone anti-tumour effect in cancer cells.

Zoldonrasib (RMC-9805)

Zoldonrasib (RMC-9805) is an orally active inhibitor of KRAS G12D. RMC-9805 inhibits Ras signalling, leading to Apoptosis in cancer cells with the KRAS G12D mutation.

Catadegbrutinib (BGB-16673)

Catadegbrutinib (BGB-16673) is an inhibitor of Bruton’s tyrosine kinase (Btk) and can be used in research for the treatment of autoimmune and inflammatory diseases.

Doxorubicin

Adriamycin (Doxorubicin, Hydroxydaunorubicin), a cytotoxic anthracycline antibiotic, is an anti-cancer chemotherapy agent, inhibits topoisomerase II with an IC50 of 2.67 μM, thus stopping DNA replication, and induces apoptosis.

Kira8

Kira8 (Ire-1 inhibitor, AMG-18) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM.

MG132 SSS

MG132 SSS(Z-Leu-Leu-Leu-al, MG132) is a potent proteasome and calpain inhibitor with IC50 of 100 nM and 1.2 μM, respectively.

Dihexa

Dihexa (PNB-0408), an oligopeptide drug, is an orally active and blood-brain barrier-permeable analogue of angiotensin IV. It binds to hepatocyte growth factor (HGF) with high affinity and potentiates its activity at its receptor, c-Met. Dihexa can also be used as a therapeutic potential in the treatment of Alzheimer’s disease.

HRS-4642

HRS-4642 is a selective inhibitor of KRAS G12D with a Kd value of 0.083 nM. It exhibits robust anti-cancer activity against KRAS G12D-mutant cancers both in vitro and in vivo.

DCZ0415

DCZ0415 is a potent inhibitor of TRIP13. DCZ0415 impairs nonhomologous end joining repair and inhibits NF-κB activity. It triggers anti-myeloma effects both in vitro, and in vivo, and primary cells obtained from myeloma patients resistant to drugs.

TAK-861 (Oveporexton)

Oveporexton (TAK-861) is a potent, orally bioavailable agonist of orexin receptor 2 (OX2R), with an EC50 of 2.5 nM in calcium mobilization assays. It induces dose-dependent membrane depolarization in histaminergic neurons within the mouse tuberomammillary nucleus (TMN) with an EC50 of 31.7 nM.

Icotinib Hydrochloride

Icotinib Hydrochloride (BPI-2009H) is a highly potent and selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) with an IC50 of 5 nM, utilised in the treatment of non-small cell lung cancer (NSCLC).

Sevabertinib (BAY 2927088)

BAY 2927088 (Sevabertinib) is the first non-covalent, potent, oral, selective, and reversible inhibitor of tyrosine kinase that potently inhibits mutant HER2 and mutant EGFR in preclinical models. It targets Exon 20 insertions in non-small-cell lung carcinoma (NSCLC) patients.

Furimazine (PBI 3939)

Furimazine (PBI 3939) is a synthetic imidazopyrazinone compound that serves as a substrate for the NanoLuc luciferase (Nluc) enzyme. When combined with Nluc, Furimazine produces exceptionally bright bioluminescent signals in mammalian cells, significantly enhancing the sensitivity of bioluminescence imaging (BLI) applications.

ERAS-0015

ERAS-0015(JYP0015) is a tricomplex inhibitor of panRAS(ON) targeting of active RAS, it binds to Cyclophilin A (CYPA) to form a high-affinity complex that sterically occludes RAS–effector interactions. It exhibits potential for research in RAS-mutant solid tumours.

Sunvozertinib

Sunvozertinib (DZD9008) is an oral, potent, and selective inhibitor of ErbBs (EGFR or Her2), particularly mutant forms of ErbBs. It also inhibits EGFR exon 20 NPH insertion, EGFR exon 20 ASV insertion, EGFR L858R and T790M mutations, Her2 exon 20 YVMA, and EGFR WT A431, with IC50 values of 20.4 nM, 20.4 nM, 1.1 nM, 7.5 nM, and 80.4 nM, respectively.

RMC5127

RMC-5127 is an orally bioavailable, mutant-selective tri-complex inhibitor of the GTP-bound (ON) form of RAS^G12V. It non-covalently binds cyclophilin A (CypA) to form a binary complex that creates a high-affinity tri-complex with RAS^G12V(ON), sterically blocking effector binding and potently suppressing RAS signaling. It exhibits CNS penetration and induces robust anti-tumor activity in KRAS^G12V-mutant NSCLC, PDAC, and CRC xenograft models.

VT3989

VT3989 (YAP/TAZ inhibitor-3) is a potent and selective oral inhibitor of TEAD auto-palmitoylation, blocking its interaction with yes-associated protein (YAP). It exhibits antitumor activity and shows potential for treating mesothelioma and solid tumours with NF2 mutations.

Semaglutide Sodium

Semaglutide Sodium (Rybelsus, Ozempic, NN9535, OG217SC, NNC 0113-0217), a long-acting glucagon-like peptide 1 (GLP-1) analogue, is a GLP-1 receptor agonist with the potential for the treatment of type 2 diabetes mellitus (T2DM).

MMAF (Monomethylauristatin F)

MMAF (Monomethylauristatin F) is a synthetic antineoplastic agent and a potent inhibitor of tubulin polymerization. MMAF (Monomethylauristatin F) is applied as a cytotoxic component of antibody-drug conjugates (ADCs) such as vorsetuzumab mafodotin, ABT-414 and SGN-CD19A.

Olitigaltin (TD139)

Olitigaltin (TD-139, GB0-139) is a potent and selective inhibitor of galectin-3 with Kd of 0.036 µM over galectin-1 and galectin-7 with Kd of 2.2 µM and 32 µM, respectively. TD-139 is used potentially for the treatment of idiopathic pulmonary fibrosis (IPF).

ISRIB

ISRIB is an integrated stress response (ISR) inhibitor that potently reverses the effects of eukaryotic initiation factor 2α (eIF2α) phosphorylation.

Tegatrabetan (BC-2059)

Tegatrabetan (BC2059, Tegavivint) is an antagonist of β-Catenin. Tegatrabetan (BC2059) treatment disrupts the binding of β-catenin with the scaffold protein transducin β-like 1 (TBL1) and proteasomal degradation and declines in the nuclear levels of β-catenin.

Navitoclax (ABT-263)

Navitoclax (ABT-263) is a potent inhibitor of Bcl-xL, Bcl-2 and Bcl-w with K_i of ", "0.5 nM, ", "1 nM and ", "1 nM in cell-free assays, but binds more weakly to Mcl-1 and A1. Phase 2.

ABT-737

ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM in cell-free assays, respectively; no inhibition observed against Mcl-1, Bcl-B or Bfl-1. ABT-737 induces mitochondrial pathway apoptosis and mitophagy. Phase 2.

Axitinib (AG-013736)

Axitinib is a multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ and c-Kit with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM in Porcine aorta endothelial cells, respectively.

Roxadustat (FG-4592)

Roxadustat (FG-4592) is an HIF-α prolyl hydroxylase inhibitor in a cell-free assay, stabilises HIF-2 and induces EPO production. Roxadustat potentiates RSL3 induced ferroptosis. Phase 3.

AZD6244 (Selumetinib)

Selumetinib (AZD6244, ARRY-142886) is a potent, highly selective MEK inhibitor with IC50 of 14 nM for MEK1 and Kd value of 530 nM for MEK2. It also inhibits ERK1/2 phosphorylation with IC50 of 10 nM, no inhibition to p38α, MKK6, EGFR, ErbB2, ERK2, B-Raf, etc. Selumetinib suppresses cell proliferation, migration and triggers apoptosis. Phase 3.

BIBF 1120 (Nintedanib)

Nintedanib is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM in cell-free assays. Phase 3.

Afatinib (BIBW2992)

Afatinib inhibits EGFR/ErbB irreversibly in vitro with IC50 of 0.5, 0.4, 10, 14, 1 nM for EGFR^wt, EGFR^L858R, EGFR^L858R/T790M ErbB2 (HER2) and ErbB4 (HER4), respectively. Afatinib induces autophagy.

BMS-536924

BMS-536924 (CS-0117) is an ATP-competitive IGF-1R/IR inhibitor with IC50 of 100 nM/73 nM, modest activity for Mek, Fak, and Lck with very little activity for Akt1, MAPK1/2.

Bortezomib

Bortezomib is a potent 20S proteasome inhibitor with K_i of 0.6 nM. It exhibits favourable selectivity towards tumour cells over normal cells. Bortezomib (PS-341) inhibits NF-κB and induces ERK phosphorylation to suppress Cathepsin B and inhibit the catalytic process of autophagy in ovarian cancer and other solid tumours.

Dasatinib (BMS-354825)

Dasatinib is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM in cell-free assays, respectively. Dasatinib induces autophagy and apoptosis with anti-tumor activity.

Erlotinib (CP-358774) Hydrochloride

Erlotinib HCl is an EGFR inhibitor with an IC50 of 2 nM in cell-free assays, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.

Gefitinib (ZD1839)

Gefitinib is an EGFR inhibitor for Tyr1173, Tyr992, Tyr1173 and Tyr992 in the NR6wtEGFR and NR6W cells with IC50 of 37 nM, 37nM, 26 nM and 57 nM, respectively. Gefitinib promotes autophagy and apoptosis of lung cancer cells via blockade of the PI3K/AKT/mTOR pathway.

CC-5013 (Lenalidomide)

Lenalidomide is a TNF-α secretion inhibitor with IC50 of 13 nM in PBMCs. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide promotes cleaved caspase-3 expression and inhibit VEGF expression and induces apoptosis.

Panobinostat (LBH589)

Panobinostat (LBH589, NVP-LBH589) is a novel broad-spectrum HDAC inhibitor with IC50 of 5 nM in a cell-free assay. Panobinostat (LBH589) induces autophagy and apoptosis. Panobinostat effectively disrupts HIV latency in vivo. Phase 3.

PD0325901 (Mirdametinib)

Mirdametinib (PD0325901) is a selective and non ATP-competitive MEK inhibitor with IC50 of 0.33 nM in cell-free assays, roughly 500-fold more potent than CI-1040 on phosphorylation of ERK1 and ERK2. Phase 2.

Rapamycin (Sirolimus)

Rapamycin is a specific mTOR inhibitor with IC50 of ~0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an Autophagy activator and an immunosuppressant.

Trichostatin A (TSA)

TSA (Trichostatin A) is an HDAC inhibitor with an IC50 of ~1.8 nM in cell-free assays.

Vorinostat (SAHA)

Vorinostat (SAHA) is an HDAC inhibitor with an IC50 of ~10 nM in a cell-free assay. Vorinostat abrogates productive HPV-18 DNA amplification.

Y-27632 Dihydrochloride

Y-27632 2HCl is a selective ROCK1 and ROCK2 inhibitor with a K_i of 140 nM and 300nM in a cell-free assay, exhibits >200-fold selectivity over other kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK.

Entinostat (MS-275)

Entinostat (MS-275, SNDX-275) strongly inhibits HDAC1 and HDAC3 with IC50 of 0.51 μM and 1.7 μM in cell-free assays, compared with HDACs 4, 6, 8, and 10. Entinostat induces autophagy and apoptosis. Phase 3.

Enzastaurin

Enzastaurin is a potent PKCβ selective inhibitor with IC50 of 6 nM in cell-free assays, 6- to 20-fold selectivity against PKCα, PKCγ and PKCε. Phase 3.

AZD2281 (Olaparib)

Olaparib (AZD2281, KU0059436) is a selective inhibitor of PARP1/2 with an IC50 of 5 nM/1 nM in cell-free assays, 300-times less effective against tankyrase-1. Olaparib induces significant Autophagy that is associated with Mitophagy in cells with BRCA mutations.

Nutlin-3

Nutlin-3 is a potent and selective Mdm2 (RING finger-dependent ubiquitin protein ligase for itself and p53) antagonist with an IC50 of 90 nM in a cell-free assay; it stabilises p73 in p53-deficient cells.

SB431542

SB431542 is a potent and selective inhibitor of ALK5 with IC50 of 94 nM in a cell-free assay, 100-fold more selective for ALK5 than p38 MAPK and other kinases.

SB203580 (Adezmapimod)

Adezmapimod (SB203580, RWJ 64809, PB 203580) is a p38 MAPK inhibitor with IC50 of 0.3-0.5 μM in THP-1 cells, 10-fold less sensitive to SAPK3(106T) and SAPK4(106T) and blocks PKB phosphorylation with IC50 of 3-5 μM. SB203580 induces mitophagy and autophagy.

SB202190

SB202190 is a potent p38 MAPK inhibitor targeting p38α/β with IC50 of 50 nM/100 nM in cell-free assays, sometimes used instead of SB 203580 to investigate potential roles for SAPK2a/p38 in vivo. SB202190 inhibits endothelial cell apoptosis via induction of autophagy and heme oxygenase-1. SB202190 significantly suppresses Erastin‐dependent ferroptosis.

MK-2206 Dihydrochloride

MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM in cell-free assays, respectively; no inhibitory activities against 250 other protein kinases observed. MK-2206 2HCl induces autophagy and apoptosis in cancer cells. Phase 2.

Vismodegib (GDC-0449)

Vismodegib (GDC-0449) is a potent, novel and specific hedgehog inhibitor with an IC50 of 3 nM and also inhibits P-gp with an IC50 of 3.0 μM in a cell-free assay.

Belinostat (PXD101)

Belinostat is a novel HDAC inhibitor with IC50 of 27 nM in a cell-free assay, with activity demonstrated in cisplatin-resistant tumours. Belinostat (PXD101) induces autophagy.

Linsitinib (OSI-906)

Linsitinib (OSI-906) is a selective inhibitor of IGF-1R with IC50 of 35 nM in cell-free assays; modestly potent to InsR with IC50 of 75 nM, and no activity towards Abl, ALK, BTK, EGFR, FGFR1/2, PKA etc. Phase 3.

Quisinostat (JNJ-26481585) Dihydrochloride

Quisinostat (JNJ-26481585) 2HCl is a novel second-generation HDAC inhibitor with highest potency for HDAC1 with IC50 of 0.11 nM in a cell-free assay, modest potent to HDACs 2, 4, 10, and 11; greater than 30-fold selectivity against HDACs 3, 5, 8, and 9 and lowest potency to HDACs 6 and 7. Phase 2.

GDC-0879

GDC-0879 (AR-00341677) is a novel, potent, and selective B-Raf inhibitor with IC50 of 0.13 nM in A375 and Colo205 cells with activity against c-Raf as well; no inhibition known to other protein kinases.

LY294002

LY294002 (SF 1101, NSC 697286) is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation. It not only binds to class I PI3Ks and other PI3K-related kinases, but also to novel targets seemingly unrelated to the PI3K family. LY294002 also inhibits CK2 with IC50 of 98 nM. LY294002 is a non-specific DNA-PKcs inhibitor and activates autophagy and apoptosis.

Varespladib (LY315920)

Varespladib (LY315920) is a potent and selective human non-pancreatic secretory phospholipase A2 (hnsPLA) inhibitor with IC50 of 7 nM. Phase 3.

PD-0332991 (Palbociclib) Hydrochloride

Palbociclib (PD-0332991) HCl is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays, respectively. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3.

XL147 analogue

XL147 analogue (SAR245408) is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ with IC50 of 39 nM/36 nM/23 nM in cell-free assays, less potent to PI3Kβ. XL147 analogue induces apoptosis. Phase 1/2.

Cabozantinib (XL184)

Cabozantinib (XL184) is a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively. Cabozantinib induces PUMA-dependent apoptosis in colon cancer cells via AKT/GSK-3β/NF-κB signalling pathway.

RAD001 (Everolimus)

Everolimus is an mTOR inhibitor of FKBP12 with IC50 of 1.6-2.4 nM in a cell-free assay. Everolimus induces cell apoptosis and autophagy and inhibits tumor cells proliferation.

SRT 1720 Hydrochloride

SRT1720 HCl is a selective SIRT1 activator with EC50 of 0.16 μM in a cell-free assay, but is >230-fold less potent for SIRT2 and SIRT3. SRT1720 induces Autophagy.

Alisertib (MLN8237)

Alisertib (MLN8237) is a selective Aurora A inhibitor with an IC50 of 1.2 nM in a cell-free assay. It has >200-fold higher selectivity for Aurora A than Aurora B. Alisertib induces cell cycle arrest, apoptosis and autophagy. Phase 3.

Tanespimycin (17-AAG)

Tanespimycin (17-AAG, CP127374, NSC-330507, KOS 953) is a potent HSP90 inhibitor with IC50 of 5 nM in a cell-free assay, having a 100-fold higher binding affinity for HSP90 derived from tumour cells than HSP90 from normal cells. Tanespimycin (17-AAG) induces apoptosis, necrosis, autophagy and mitophagy. Phase 3.

Ivacaftor (VX-770)

Ivacaftor (VX-770) is a selective potentiator of CFTR targeting G551D-CFTR and F508del-CFTR with EC50 of 100 nM and 25 nM in fisher rat thyroid cells, respectively.

Cyclopamine (11-Deoxojervine)

Cyclopamine (11-deoxojervine) is a specific Hedgehog (Hh) signaling pathway antagonist of Smoothened (Smo) with an IC50 of 46 nM in TM3Hh12 cells.

Barasertib-HQPA (AZD2811)

Defosbarasertib (AZD1152-HQPA, AZD2811, INH-34, Barasertib-HQPA) is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay, ~3700 fold more selective for Aurora B over Aurora A. Phase 1.

Docetaxel

Docetaxel, an analog of paclitaxel, is an inhibitor of depolymerisation of microtubules by binding to stabilized microtubules.

Gemcitabine Hydrochloride

Gemcitabine is a pyrimidine nucleoside analog antitumor drug that can inhibit DNA synthesis and repair, leading to cell Autophagy and apoptosis. It is mainly used to treat various solid tumors such as pancreatic cancer and non-small cell lung cancer, and is often combined with chemotherapy to enhance efficacy.

Paclitaxel

Paclitaxel is a microtubule polymer stabilizer with an IC50 of 0.1 pM in human endothelial cells. Paclitaxel can cause both mitotic arrest and apoptotic cell death. Paclitaxel also induces Autophagy.

E7080 (Lenvatinib)

Lenvatinib is a multi-target inhibitor, mostly for VEGFR2(KDR)/VEGFR3(Flt-4) with IC50 of 4 nM/5.2 nM, less potent against VEGFR1/Flt-1, ~10-fold more selective for VEGFR2/3 against FGFR1, PDGFRα/β in cell-free assays. Lenvatinib (E7080) also inhibits FGFR1-4, PDGFR, Kit (c-Kit), RET (c-RET), and shows potent antitumor activities. Phase 3.

Cisplatin

Cisplatin is an inorganic platinum complex, which is able to inhibit DNA synthesis by conforming DNA adducts in tumour cells. Cisplatin activates ferroptosis and induces autophagy.Solutions are unstable and should be fresh-prepared.DMSO is not recommended to dissolve platinum-based drugs, which can easily lead to drug inactivation.

XAV-939

XAV-939 (NVP-XAV939) selectively inhibits Wnt/β-catenin-mediated transcription through tankyrase1/2 inhibition with IC50 of 11 nM/4 nM in cell-free assays, regulates axin levels and does not affect CRE, NF-κB or TGF-β.

Aprepitant

Aprepitant is a potent and selective neurokinin-1 receptor antagonist with IC50 of 0.1 nM. Aprepitant reduces levels of pro-inflammatory cytokines including G-CSF, IL-6, IL-8 and TNFα. Aprepitant inhibits HIV infection of human macrophages.

Bicalutamide

Bicalutamide is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line. Bicalutamide promotes autophagy.

Fulvestrant (ICI-182780)

Fulvestrant is an estrogen receptor (ER) antagonist with IC50 of 0.94 nM in a cell-free assay. Fulvestrant also induces autophagy and apoptosis and has antitumor activity.

Irinotecan (CPT-11)

Irinotecan is a topoisomerase I inhibitor for LoVo cells and HT-29 cells with IC50 of 15.8 μM and 5.17 μM, respectively.

Decitabine

Decitabine is a DNA methyltransferase inhibitor, incorporating into DNA and resulting in hypomethylation of DNA and intra-S-phase arrest of DNA replication. It is used to treat myelodysplastic syndrome (MDS). Decitabine induces cell cycle arrest and apoptosis in various cancer cell lines.

Doxorubicin (Adriamycin) Hydrochloride

Doxorubicin Hydrochloride is an antibiotic agent and DNA Topoisomerase II Inhibitor with IC50 of 2.67 μM against human DNA topoisomerase II. This compound reduces basal phosphorylation of AMPK and is used in the concomitant treatment of HIV-infected patients but is found to be at high risk of HBV reactivation. This product may precipitate when dissolved in PBS solution. It is recommended to prepare the stock solution in pure water and dilute with either pure water or saline to obtain the working solution. It can be used to induce animal models of kidney disease.

5-Fluorouracil (5-FU)

5-FU (5-Fluorouracil) is a DNA/RNA synthesis inhibitor, which interrupts nucleotide synthetic by inhibiting thymidylate synthase (TS) in tumour cells. Fluorouracil induces apoptosis and can be used in the treatment of HIV.

Methotrexate

Methotrexate, an analog of folic acid, is a nonspecific inhibitor of the dihydrofolate reductase (DHFR) of bacteria and cancerous cells as well as normal cells. It forms an inactive ternary complex with DHFR and NADPH. Methotrexate (MTX) induces apoptosis.

Nelarabine

Nelarabine (506U78,Arranon) is a purine nucleoside analog and DNA synthesis inhibitor with IC50 from 0.067-2.15 μM in tumour cells.

Bleomycin sulfate

Bleomycin sulfate is a DNA synthesis inhibitor and a glycopeptide antibiotic, as well as an anticancer agent for squamous cell carcinomas (SCC) with an IC50 of 4 nM in UT-SCC-19A cells. This chemical can be used to induce animal models of pulmonary fibrosis.

Carboplatin

Carboplatin, a derivative of CDDP, is a DNA synthesis inhibitor which binds to DNA, inhibits replication and transcription and induces cell death and interfers with the cell's repair mechanism in A2780, SKOV-3, IGROV-1, and HX62 cells. It induces the formation of DNA interstrand crosslinks and DNA-protein crosslinks. Solutions are unstable and should be fresh-prepared.DMSO is not recommended to dissolve platinum-based drugs, which can easily lead to drug inactivation.

Cyclophosphamide

Cyclophosphamide (NSC 26271, Endoxan, Cytoxan, Neosar, Procytox, Revimmune, Cytophosphane) is a nitrogen mustard alkylating agent from the oxazophorines group.

Oxaliplatin

Oxaliplatin is a DNA alkylating agent that activates autophagy. Oxaliplatin inhibits DNA synthesis by conforming DNA adducts in RT4, TCCSUP, A2780, HT-29, U-373MG, U-87MG, SK-MEL-2, and HT-144 cells.Solutions are unstable and should be fresh-prepared.DMSO is not recommended to dissolve platinum-based drugs, which can easily lead to drug inactivation.

Etoposide

Etoposide is a semisynthetic derivative of podophyllotoxin, which inhibits DNA synthesis via topoisomerase II inhibition activity which enhances double-strand and single-strand cleavage of DNA and reversibly inhibits repair by topoisomerase II binding. Etoposide induces autophagy, mitophagy and apoptosis.

Fludarabine (NSC 118218) Phosphate

Fludarabine Phosphate is an analogue of adenosine and deoxyadenosine, which is able to compete with dATP for incorporation into DNA and inhibit DNA synthesis.

TMZ(Temozolomide)

TMZ(Temozolomide) is a monofunctional SN-1 alkylating agent that can modify nitrogen atoms in the DNA ring and the extracyclic oxygen group, chemically converted to MTIC and degrades to methyldiazonium cation, which transfers methyl groups to DNA at physiologic pH. A DNA damage inducer in L-1210 and L-1210/BCNU cells. Temozolomide induces apoptosis and exhibits antitumor activity.

Tamoxifen

Tamoxifen is an orally active, selective estrogen receptor modulator (SERM) which exhibits both estrogenic agonist and antagonist effects. It blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity.

Vincristine (Leurocristine) Sulfate

Vincristine sulfate is an inhibitor of polymerization of microtubules by binding to tubulin with IC50 of 32 μM in a cell-free assay. Vincristine sulfate induces apoptosis.

JNJ-7706621

JNJ-7706621 is a pan-CDK inhibitor with the highest potency on CDK1/2 with IC50 of 9 nM/4 nM and showing >6-fold selectivity for CDK1/2 than CDK3/4/6 in cell-free assays. It also potently inhibits Aurora A/B and has no activity on Plk1 and Wee1.

MDV3100 (Enzalutamide)

Enzalutamide is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells. Enzalutamide is shown to increase autophagy.

CHIR-99021 (Laduviglusib)

Laduviglusib (CHIR-99021, CT99021) is a GSK-3α and GSK-3β inhibitor with IC50 of 10 nM and 6.7 nM, respectively. CHIR99201 does not exhibit cross-reactivity against cyclin-dependent kinases (CDKs) and shows a 350-fold selectivity toward GSK-3β compared to CDKs. CHIR99021 functions as a Wnt/β-catenin activator and induces autophagy.

PD173074

PD173074 is a potent FGFR1 inhibitor with IC50 of ~25 nM and also inhibits VEGFR2 with IC50 of 100-200 nM in cell-free assays, ~1000-fold selective for FGFR1 than PDGFR and c-Src. PD173074 reduces proliferation and promotes apoptosis in gastric cancer cells.

PLX4032 (Vemurafenib)

Vemurafenib (PLX4032, RG7204, RO5185426) is a novel and potent inhibitor of B-Raf^V600E with IC50 of 31 nM in cell-free assay. 10-fold selective for B-Raf^V600E over wild-type B-Raf in enzymatic assays and the cellular selectivity can exceed 100-fold. Vemurafenib (PLX4032, RG7204) induces Autophagy.

Camptothecin (CPT)

Camptothecin (CPT) is a specific inhibitor of DNA topoisomerase I (Topo I) with an IC50 of 0.68 μM in a cell-free assay. Camptothecin induces apoptosis in cancer cells via microRNA-125b-mediated mitochondrial pathways. Phase 2.

Dexamethasone

Dexamethasone is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects. Dexamethasone induces autophagy and mitophagy. Dexamethasone is tested in hospitalized patients with COVID-19 and is found to have benefits for critically ill patients.

Fluoxetine Hydrochloride (LY-110140)

Fluoxetine HCl is a selective serotonin-reuptake inhibitor (SSRI) at the neuronal membrane, used in the treatment of depression.

Heparin Sodium

Heparin sodium, a sulfated polysaccharide belonging to the family of glycosaminoglycans, has numerous important biological activities associated with its interaction with diverse proteins. Heparin is used as an anticoagulant primarily through its interaction with AT III by enhancing AT-IIImediated inhibition of blood coagulation factors, including thrombin and factor Xa. Heparin prevents the induction of autophagy.

Ruxolitinib (INCB18424)

Ruxolitinib (INCB18424) is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM in cell-free assays, >130-fold selectivity for JAK1/2 versus JAK3. This compound kills tumour cells through toxic mitophagy. It induces autophagy and enhances apoptosis.

Resveratrol (trans-Resveratrol)

Resveratrol has a wide spectrum of targets including cyclooxygenases(i.e. COX, IC50=1.1 μM), lipooxygenases（LOX, IC50=2.7 μM）, kinases, sirtuins and other proteins. It has anti-cancer, anti-inflammatory, blood-sugar-lowering and other beneficial cardiovascular effects. Resveratrol induces mitophagy/autophagy and autophagy-dependent apoptosis.

Bafilomycin A1 (Baf-A1)

Bafilomycin A1 (Baf-A1) is a vacuolar H⁺-ATPase inhibitor with IC50 of 0.44 nM. Bafilomycin A1 is found to inhibit autophagy while inducing apoptosis.

Staurosporine (STS)

Staurosporine (STS) is a potent PKC inhibitor for PKCα, PKCγ and PKCη with IC50 of 2 nM, 5 nM and 4 nM, less potent to PKCδ (20 nM), PKCε (73 nM) and little active to PKCζ (1086 nM) in cell-free assays. Also shows inhibitory activities on other kinases, such as PKA, PKG, S6K, CaMKII, etc. Phase 3.

Thiazovivin (TZV)

Thiazovivin is a novel ROCK inhibitor with IC50 of 0.5 μM in a cell-free assay, promotes hESC survival after single-cell dissociation.

SP600125

SP600125 (Nsc75890) is a broad-spectrum JNK inhibitor for JNK1, JNK2 and JNK3 with IC50 of 40 nM, 40 nM and 90 nM in cell-free assays, respectively; 10-fold greater selectivity against MKK4, 25-fold greater selectivity against MKK3, MKK6, PKB, and PKCα, and 100-fold selectivity against ERK2, p38, Chk1, EGFR etc. SP600125 is also a broad‐spectrum inhibitor of serine/threonine kinases including Aurora kinase A, FLT3 and TRKA with of IC50 of 60 nM, 90 nM and 70 nM. SP600125 inhibits autophagy and activates apoptosis.

Oligomycin A (MCH 32)

Oligomycin A (MCH 32), a dominant analogue of the isomers, is an inhibitor of mitochondrial F1FO ATP synthase which inhibits oxidative phosphorylation and all the ATP-dependent processes occurring on the coupling membrane of mitochondria. It inhibits ATP synthase by blocking its proton channel (Fo subunit), which is necessary for oxidative phosphorylation of ADP to ATP. It also induces apoptosis in a variety of cell types.

Ponatinib (AP24534)

Ponatinib is a novel, potent multi-target inhibitor of Abl, PDGFRα, VEGFR2, FGFR1 and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM and 5.4 nM in cell-free assays, respectively. Ponatinib (AP24534) inhibits autophagy.

Fludarabine

Fludarabine is a STAT1 activation inhibitor which causes a specific depletion of STAT1 protein (and mRNA) but not of other STATs. Also a DNA synthesis inhibitor in vascular smooth muscle cells. Fludarabine induces apoptosis.

Tadalafil

Tadalafil is a PDE-5 inhibitor with IC50 of 1.8 nM in a cell-free assay. Tadalafil is at least 9000 times more selective for PDE5 than most of the other families of PDEs, with the exception of PDE11. It can partial inhibits PDE11

Hesperadin

Hesperadin potently inhibits Aurora B with IC50 of 250 nM in a cell-free assay. It markedly reduces the activity of AMPK, Lck, MKK1, MAPKAP-K1, CHK1 and PHK while it does not inhibit MKK1 activity in vivo.

CP-673451

CP-673451 is a selective inhibitor of PDGFRα/β with an IC50 of 10 nM/1 nM in cell-free assays, exhibits >450-fold selectivity over other angiogenic receptors, has antiangiogenic and antitumour activity.

Vadimezan (DMXAA)

Vadimezan (DMXAA) is a vascular disrupting agents (VDA) and competitive inhibitor of DT-diaphorase with Ki of 20 μM and IC50 of 62.5 μM in cell-free assays, respectively. DMXAA (Vadimezan) is also a STING agonist with potential antineoplastic activity. DMXAA (Vadimezan) potently induces IFN-β but relatively low TNF-α expression in vitro. DMXAA (Vadimezan) has antiviral activity. Phase 3.

Telaprevir (VX-950)

Telaprevir is an HCV NS3-4A serine protease inhibitor with IC50 of 0.35 μM.

VX-809 (Lumacaftor)

Lumacaftor (VX-809, VRT 826809) acts to correct CFTR mutations common in cystic fibrosis by increasing mutant CFTR (F508del-CFTR) maturation, EC50 of 0.1 μM in fisher rat thyroid cells. Phase 3.

Pomalidomide (CC-4047)

Pomalidomide inhibits LPS-induced TNF-α release with IC50 of 13 nM in PBMCs. Pomalidomide can be utilized in PROTAC as a ligand for targeting E3 ligase and inhibiting the E3 ligase protein cereblon (CRBN). Pomalidomide promotes apoptosis and cell cycle arrest.

KU-60019

KU-60019 is an improved analogue of KU-55933, with an IC50 of 6.3 nM for ATM in cell-free assays, 270- and 1600-fold more selective for ATM than DNA-PK and ATR, and is a highly effective radiosensitizer.

RO4929097 (RG-4733)

RO4929097 (RG-4733) is a γ secretase inhibitor with IC50 of 4 nM in a cell-free assay, inhibiting cellular processing of Aβ40 and Notch with EC50 of 14 nM and 5 nM, respectively. Phase 2.

Bestatin (Ubenimex)

Bestatin (Ubenimex) is a potent aminopeptidase-B and leukotriene (LT) A4 hydrolase inhibitor, used in the treatment of acute myelocytic leukaemia.

N-Acetylcysteine (NAC chemical, N-Acetyl-L-Cysteine)

Acetylcysteine (N-acetyl-l-cysteine, NAC, N-acetylcysteine) is a ROS (reactive oxygen species) inhibitor that antagonises the activity of proteasome inhibitors. It is also a tumor necrosis factor production inhibitor. Acetylcysteine (N-acetyl-l-cysteine) suppresses TNF-induced NF-κB activation through inhibition of IκB kinases. Acetylcysteine (N-acetyl-l-cysteine) induces apoptosis via the mitochondria-dependent pathway. Acetylcysteine (N-acetyl-l-cysteine) inhibits ferroptosis and virus replication.Solutions are unstable and should be fresh-prepared.

Cytarabine

Cytarabine is an antimetabolic agent and DNA synthesis inhibitor with IC50 of 16 nM in wild-type CCRF-CEM cells. Cytarabine induces autophagy and apoptosis.

Retinoic acid (Tretinoin, Vitamin A acid)

Retinoic acid (Tretinoin) is a natural agonist of RAR agonist; it can induce granulocytic differentiation and apoptosis in acute promyelocytic leukaemia (APL) cells. Tretinoin (NSC 122758) can be used to induce animal models of osteoporosis.

Tetraethylthiuram disulfide (Disulfiram)

Disulfiram is a specific inhibitor of aldehyde-dehydrogenase (ALDH) with IC50 of 0.15 μM and 1.45 μM for hALDH1 and hALDH2, respectively. Disulfiram is used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol. Disulfiram induces apoptosis. Disulfiram is also an inhibitor of pore formation by gasdermin D (GSDMD).

Busulfan

Busulfan is a cell cycle non-specific alkylating antineoplastic agent. It causes DNA damage by cross-linking DNAs and DNA and proteins. Busulfan inhibits thioredoxin reductase activity. It also induces apoptosis. It is an immunosuppressive and myeloablative chemotherapeutic agent.Busulfan (NSC-750) can be used to induce animal models of Anemia.

17β-Estradiol

Estradiol (17β-estradiol, β-Estradiol, E2, 17β-Oestradiol) is a human sex hormone and steroid, and the primary female sex hormone. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway.

Gemcitabine

Gemcitabine, a nucleic acid synthesis inhibitor, is a very potent and specific deoxycytidine analogue, used as chemotherapy. Gemcitabine induces a potent p53-dependent apoptosis.

Pitavastatin (NK-104) Calcium

Pitavastatin calcium, a novel member of the medication class of statins, is a calcium salt formulation of pitavastatin which is a highly effective HMG-CoA reductase inhibitor. Pitavastatin Calcium attenuates AGEs-induced mitophagy via inhibition of ROS generation. Pitavastatin Calcium induces autophagy and apoptosis.

5-Azacytidine (5-Aza, Azacitidine)

Azacitidine (5-Azacytidine, 5-AzaC, Ladakamycin, AZA, 5-Aza, CC-486, NSC 102816) is a nucleoside analogue of cytidine that specifically inhibits DNA methylation by trapping DNA methyltransferases. Azacitidine induces mitochondrial apoptosis and autophagy.

Verteporfin

Verteporfin is a small molecule that inhibits TEAD–YAP association and YAP-induced liver overgrowth. It is also a potent second-generation photosensitizing agent derived from porphyrin. Verteporfin is an autophagy inhibitor. Verteporfin inhibits cell proliferation and induces apoptosis.

Simvastatin (MK-733)

Simvastatin is a competitive inhibitor of HMG-CoA reductase with K_i of 0.1-0.2 nM in cell-free assays. Simvastatin induces ferroptosis, mitophagy, autophagy and apoptosis.

Dipyridamole

Dipyridamole is a phosphodiesterase inhibitor that blocks uptake and Metabolism of adenosine by erythrocytes and vascular endothelial cells.

Hydroxyurea

Hydroxyurea is an antineoplastic agent that inhibits DNA synthesis through the inhibition of ribonucleoside diphosphate reductase. Hydroxyurea activates apoptosis and autophagy. Hydroxyurea is used to treat HIV infection.

Nicotinamide (Niacinamide)

Nicotinamide, a water-soluble vitamin, is an active component of coenzymes NAD and NADP, and also acts as an inhibitor of sirtuins.

Metformin Hydrochloride

Metformin Hydrochloride (1,1-Dimethylbiguanide Hydrochloride) is a highly effective Antihyperglycemic Agent, which primarily decreases hyperglycemia in hepatocytes by suppressing hepatic gluconeogenesis (glucose production by the liver). It also promotes Mitophagy in mononuclear cells and induces apoptosis of lung cancer cells through activating the JNK/p38 MAPK pathway and GADD153.

Maraviroc (UK-427857)

Maraviroc is a CCR5 antagonist for MIP-1α, MIP-1β and RANTES with IC50 of 3.3 nM, 7.2 nM and 5.2 nM in cell-free assays, respectively. Maraviroc is used in the treatment of HIV infection.

Gabapentin

Gabapentin is a GABA analogue, used to treat seizures and neuropathic pain.

Neratinib (HKI-272)

Neratinib is a highly selective HER2 and EGFR inhibitor with IC50 of 59 nM and 92 nM in cell-free assays; weakly inhibits KDR and Src, no significant inhibition to Akt, CDK1/2/4, IKK-2, MK-2, PDK1, c-Raf and c-Met. Phase 3.

ITF-2357 (Givinostat) Hydrochloride Monohydrate

Givinostat (ITF2357) is a potent HDAC inhibitor for maize HD2, HD1B and HD1A with IC50 of 10 nM, 7.5 nM and 16 nM in cell-free assays. Phase 2.

MLN2238 (Ixazomib)

Ixazomib (MLN2238) inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with IC50 and K_i of 3.4 nM and 0.93 nM in cell-free assays, respectively, also inhibits the caspase-like (β1) and trypsin-like (β2) proteolytic sites, with IC50 of 31 and 3500 nM. Ixazomib (MLN2238) induces autophagy. Phase 3.

BGJ398 (Infigratinib)

Infigratinib (BGJ398) is a potent and selective FGFR inhibitor for FGFR1/2/3 with IC50 of 0.9 nM/1.4 nM/1 nM in cell-free assays, >40-fold selective for FGFR versus FGFR4 and VEGFR2, and little activity to Abl, Fyn, Kit, Lck, Lyn and Yes. Phase 2.

DAPT

DAPT is a novel γ-secretase inhibitor, which inhibits Aβ production with IC50 of 20 nM in HEK 293 cells. DAPT enhances the apoptosis of human tongue carcinoma cells and regulates autophagy.

CAL-101 (Idelalisib)

Idelalisib (CAL-101) is a selective p110δ inhibitor with IC50 of 2.5 nM in cell-free assays; shown to have 40- to 300-fold greater selectivity for p110δ than p110α/β/γ, and 400- to 4000-fold more selectivity to p110δ than C2β, hVPS34, DNA-PK and mTOR. Idelalisib also stimulates autophagy.

Galunisertib (LY2157299)

Galunisertib (LY2157299) is a potent TGFβ receptor I (TβRI / ALK5) inhibitor with IC50 of 56 nM in a cell-free assay. Phase 2/3.

Volasertib (BI6727)

Volasertib is a highly potent Plk1 inhibitor with IC50 of 0.87 nM in a cell-free assay. It shows 6- and 65-fold greater selectivity against Plk2 and Plk3. Volasertib induces cell cycle arrest and apoptosis in various cancer cells. Phase 3.

Buparlisib (BKM120)

Buparlisib (BKM120, NVP-BKM120) is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM in cell-free assays, respectively. Reduced potency against VPS34, mTOR, DNAPK, with little activity to PI4Kβ. Buparlisib induces apoptosis. Phase 2.

Cyclosporin A

Cyclosporin A, a non-polar cyclic oligopeptide, is an immunosuppressive agent that binds to cyclophilin and then inhibits calcineurin with IC50 of 7 nM in a cell-free assay. Cyclosporin A is generally given following transplant surgery to prevent rejection and has been used to test its toxic effect on a perfused 3D proximal tubule model. Cyclosporin A (NSC 290193) can be used to induce animal models of Chronic Rejection of Liver Transplantation.

Quercetin (Sophoretin)

Quercetin, a natural flavonoid present in vegetables, fruit and wine, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4-5.4 μM. Quercetin induces mitophagy, apoptosis and protective autophagy. Phase 4.

Forskolin (Colforsin)

Forskolin (Colforsin) is a ubiquitous activator of eukaryotic adenylyl cyclase (AC) in a wide variety of cell types, commonly used to raise levels of cAMP in the study and research of cell physiology. Forskolin also activates PXR and FXR activity. Forskolin stimulates autophagy.

Clindamycin HCl

Clindamycin HCl inhibits protein synthesis by acting on the 50S ribosomal, used for the treatment of Bacterial infections.

Imatinib (STI571)

Imatinib is a multi-target inhibitor of tyrosine kinase with inhibition for v-Abl, c-Kit and PDGFR, IC50 values are 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib (STI571) induces autophagy.

Novobiocin Sodium (Cathomycin, Albamycin)

Novobiocin Sodium (NSC 2382, Albamycin, Cathomycin) is an aminocoumarin antibiotic that targets bacterial DNA gyrase (TopoIV), used to treat susceptible gram positive bacteria.

NAD+ (β-DPN)

NAD+ (β-DPN, β-NAD, β-Nicotinamide Adenine Dinucleotide, nicotinamide adenine dinucleotide) is a coenzyme composed of ribosylnicotinamide 5'-diphosphate coupled to adenosine 5'-phosphate by pyrophosphate linkage.

LDN-193189

LDN-193189 (DM3189) is a selective BMP signalling inhibitor, inhibits the ALK1, ALK2, ALK3 and ALK6 with IC50s of 0.8 nM, 0.8 nM, 5.3 nM and 16.7 nM in the kinase assay, respectively. LDN-193189 inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50s of 5 nM and 30 nM in C2C12 cells, respectively, exhibits 200-fold selectivity for BMP versus TGF-beta/Smad. For cell testing, the water-soluble S7507 LDN-193189 2HCl is recommended.This product has poor solubility, animal experiments are available, cell experiments please choose carefully!

MG132

MG132 ((S,R,S)-(-)-MG132, Z-Leu-D-Leu-Leu-al) is a potent proteasome (ChTL, TL, and PGPH) inhibitor. MG132 also inhibits calpain (IC50=1.2 μM). MG132 can be used to induce animal models of Parkinson’s disease.

Omecamtiv mecarbil (CK-1827452)

Omecamtiv mecarbil (CK-1827452) is a specific cardiac myosin activator and a clinical drug for left ventricular systolic heart failure. Phase 2.

Tubastatin A Hydrochloride

Tubastatin A HCl is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. It is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more).

NU7441 (KU-57788)

NU7441 (KU-57788) is a highly potent and selective DNA-PK inhibitor with IC50 of 14 nM and also inhibits mTOR and PI3K with IC50 of 1.7 μM and 5 μM in cell-free assays, respectively. It reduces the frequency of NHEJ while increasing the rate of HDR following Cas9-mediated DNA cleavage.

ICG-001

ICG-001 antagonizes Wnt/β-catenin/TCF-mediated transcription and specifically binds to CREB-binding protein (CBP) with IC50 of 3 μM, but is not the related transcriptional coactivator p300. ICG-001 induces apoptosis.

GSK1349572 (Dolutegravir)

Dolutegravir is a two-metal-binding HIV Integrase inhibitor with IC50 of 2.7 nM in a cell-free assay, modest activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S/Q148H.

Trametinib (GSK1120212)

Trametinib (GSK1120212, JTP-74057) is a highly specific and potent MEK1/2 inhibitor with IC50 of 0.92 nM/1.8 nM in cell-free assays, no inhibition of the kinase activities of c-Raf, B-Raf, ERK1/2. Trametinib activates autophagy and induces apoptosis.

Ibrutinib (PCI-32765)

Ibrutinib is a potent and highly selective Brutons tyrosine kinase (Btk) inhibitor with IC50 of 0.5 nM in cell-free assays, modestly potent to Bmx, CSK, FGR, BRK, HCK, less potent to EGFR, Yes, ErbB2, JAK3, etc. Ibrutinib is applicable as a Btk ligand in the synthesis of a series of PROTACs including P13I.

CX-5461 (Pidnarulex)

Pidnarulex (CX-5461) is an inhibitor of rRNA synthesis, selectively inhibits Pol I-driven transcription of rRNA with IC50 of 142 nM in HCT-116, A375, and MIA PaCa-2 cells, has no effect on Pol II, and possesses 250- to 300-fold selectivity for inhibition of rRNA transcription versus DNA replication and protein translation.

LY2109761

LY2109761 is a novel selective TGF-β receptor type I/II (TβRI/II) dual inhibitor with K_i of 38 nM and 300 nM in a cell-free assay, respectively; shown to negatively affect the phosphorylation of Smad2. LY2109761 blocks autophagy and induces apoptosis.

LY411575

LY411575 is a potent γ-secretase inhibitor with IC50 of 0.078 nM/0.082 nM (membrane/cell-based), also inhibits Notch cleavage with IC50 of 0.39 nM in APP or NΔE expressing HEK293 cells. LY411575 induces Apoptosis.

PH-797804

PH-797804 is a novel pyridinone inhibitor of p38α with IC50 of 26 nM in a cell-free assay; 4-fold more selective versus p38β and does not inhibit JNK2. Phase 2.

Niraparib (MK-4827)

Niraparib (MK-4827) is a selective inhibitor of PARP1/2 with IC50 of 3.8 nM/2.1 nM, with great activity in cancer cells with mutant BRCA-1 and BRCA-2. It is >330-fold selective against PARP3, V-PARP and Tank1. Niraparib can form PARP–DNA complexes resulting in DNA damage, apoptosis, and cell death. Phase 3.

Fimepinostat (CUDC-907)

CUDC-907 is a dual PI3K and HDAC inhibitor for PI3Kα and HDAC1/2/3/10 with IC50 of 19 nM and 1.7 nM/5 nM/1.8 nM/2.8 nM, respectively. CUDC-907 induces cell cycle arrest and apoptosis in breast cancer cells. Phase 1.

Canagliflozin (JNJ-28431754)

Canagliflozin (TA 7284, JNJ 28431754) is a highly potent and selective SGLT2 inhibitor for hSGLT2 with IC50 of 2.2 nM in a cell-free assay, exhibits 413-fold selectivity over hSGLT1.

Alectinib (CH5424802)

Alectinib is a potent ALK inhibitor with IC50 of 1.9 nM in cell-free assays, sensitive to L1196M mutation and higher selectivity for ALK than PF-02341066, NVP-TAE684 and PHA-E429.

Dinaciclib (SCH 727965)

Dinaciclib is a novel and potent CDK inhibitor for CDK2, CDK5, CDK1 and CDK9 with IC50 of 1 nM, 1 nM, 3 nM and 4 nM in cell-free assays, respectively. It also blocks thymidine (dThd) DNA incorporation. Dinaciclib induces apoptosis through the activation of Caspase 8 and 9. Phase 3.

Nocodazole

Nocodazole is a rapidly-reversible inhibitor of microtubule polymerisation, also inhibits Abl, Abl(E255K) and Abl(T315I) with IC50 of 0.21 μM, 0.53 μM and 0.64 μM in cell-free assays, respectively. Nocodazole induces apoptosis.

CPI-613 (Devimistat)

Devimistat (CPI-613), a lipoate analog, inhibits mitochondrial enzymes pyruvate dehydrogenase (PDH) and α-ketoglutarate dehydrogenase in NCI-H460 cell line, disrupts tumor cell mitochondrial metabolism. CPI-613 induces apoptosis in pancreatic cancer cells. Phase 2.

GW4064

GW4064 is an agonist of farnesoid X receptor (FXR) with EC50 of 65 nM in CV1 cell line and displays no activity at other nuclear receptors at concentrations up to 1 μM. GW4064 stimulates Autophagy in MCF-7 cells.

FK866 (Daporinad)

Daporinad (FK866) effectively inhibits nicotinamide phosphoribosyltransferase (NMPRTase; NAMPT) with IC50 of 0.09 nM in a cell-free assay. Daporinad (FK866, APO866) triggers Autophagy. Phase 1/2.

Dabrafenib (GSK2118436)

Dabrafenib is a mutant BRAF^V600E specific inhibitor with IC50 of 0.7 nM in cell-free assays, with 7- and 9-fold less potency against B-Raf(wt) and c-Raf, respectively.

Ipatasertib (GDC-0068)

Ipatasertib (GDC-0068, RG7440) is a highly selective pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 5 nM/18 nM/8 nM in cell-free assays, 620-fold selectivity over PKA. Phase 2.

Alpelisib (BYL719)

Alpelisib (BYL719) is a potent and selective PI3Kα inhibitor with an IC50 of 5 nM in a cell-free assay, and minimal effect on PI3Kβ/γ/δ. Phase 2.

Torin 2

Torin 2 is a potent and selective mTOR inhibitor with IC50 of 0.25 nM in p53 / - MEFs cell line; 800-fold greater selectivity for mTOR than PI3K and improved pharmacokinetic properties. Inhibition of ATM/ATR/DNA-PK with EC50 of 28 nM/35 nM/118 nM,in PC3 cell lines respectively. Torin 2 decreases cell viability and induces autophagy and apoptosis.

Torin 1

Torin 1 is a potent inhibitor of mTORC1/2 with IC50 of 2 nM/10 nM in cell-free assays; exhibits 1000-fold selectivity for mTOR than PI3K.

Bemcentinib (R428)

Bemcentinib (R428, BGB324) is an inhibitor of Axl with IC50 of 14 nM, >100-fold selective for Axl versus Abl. Selectivity for Axl is also greater than Mer and Tyro3 (50-to-100- fold more selective) and InsR, EGFR, HER2, and PDGFR (100- fold more selective).

SAR131675

SAR131675 is a VEGFR3 inhibitor with IC50/K_i of 23 nM/12 nM in cell-free assays, about 50- and 10-fold more selective for VEGFR3 than VEGFR1/2, little activity against Akt1, CDKs, PLK1, EGFR, IGF-1R, c-Met, Flt2 etc.

Baricitinib (LY3009104)

Baricitinib is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM in cell-free assays, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. Baricitinib is found to reduce or interrupt the passage of the virus into target cells and is used in the treatment research for COVID-19. Phase 3.

PR-171 (Carfilzomib)

Carfilzomib (PR-171) is an irreversible Proteasome inhibitor with IC50 of <5 nM in ANBL-6 cells, displayed preferential in vitro inhibitory potency against the ChT-L activity in the β5 subunit, but little or no effect on the PGPH and T-L activities. Carfilzomib activates prosurvival Autophagy and induces cell Apoptosis.

Stemregenin 1 (SR1)

SR1 (StemRegenin 1) is an aryl hydrocarbon receptor (AhR) inhibitor with an IC50 of 127 nM in a cell-free assay.

Pirfenidone

Pirfenidone is an inhibitor for TGF-β production and TGF-β stimulated collagen production, reduces production of TNF-α and IL-1β, and also has anti-fibrotic and anti-inflammatory properties. Pirfenidone attenuates chemokine (CC motif) ligand-2 (CCL2) and CCL12 production with anti-fibrotic activity. Phase 3.

Go 6983

Go 6983 (GOE 6983, Gö 6983) is a pan-PKC inhibitor against PKCα, PKCβ, PKCγ and PKCδ with IC50 of 7 nM, 7 nM, 6 nM and 10 nM, respectively; less potent to PKCζ and inactive to PKCμ.

Laduviglusib (CHIR-99021) Hydrochloride

Laduviglusib (CHIR-99021; CT99021) HCl is hydrochloride of CHIR-99021, which is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM; CHIR-99021 shows greater than 500-fold selectivity for GSK-3 versus its closest homologs Cdc2 and ERK2. CHIR-99021 is a potent pharmacological activators of the Wnt/beta-catenin signaling pathway. CHIR-99021 significantly rescues light-induced autophagy and augments GR, RORα and autophagy-related proteins.

Pifithrin-α (PFTα) Hhydrobromide

Pifithrin-α is an inhibitor of p53, inhibiting p53-dependent transactivation of p53-responsive genes. Pifithrin-α is also a potent agonist of the aryl hydrocarbon receptor (AhR).

Nicotinamide Riboside Chloride (NR-Cl)

Nicotinamide Riboside Chloride is the chloride salt form of nicotinamide riboside (NR). NR is a new form pyridine-nucleoside of vitamin B3 that functions as a precursor to nicotinamide adenine dinucleotide (NAD) or NAD⁺. Nicotinamide Riboside Chloride is a crystal form of Nicotinamide riboside (NR) chloride. Nicotinamide Riboside Chloride increases NAD[+] levels and activates SIRT1 and SIRT3, culminating in enhanced oxidative metabolism and protection against high fat diet-induced metabolic abnormalities. Nicotinamide Riboside Chloride is used in dietary supplements.

Romidepsin (FK228)

Romidepsin (FK228, Depsipeptide, FR 901228, NSC 630176) is a potent HDAC1 and HDAC2 inhibitor with IC50 of 36 nM and 47 nM in cell-free assays, respectively. Romidepsin (FK228/depsipeptide) controls growth and induces apoptosis in neuroblastoma tumour cells.

Pravastatin (CS-514) Sodium

Pravastatin sodium (CS-514) is an HMG-CoA Reductase inhibitor against sterol synthesis with IC50 of 5.6 μM.

Purmorphamine

Purmorphamine (Shh Signaling Antagonist VI), which directly binds and activates Smoothened, blocks BODIPY-cyclopamine binding to Smo with IC50 of ~ 1.5 μM in HEK293T cell and also is an inducer of osteoblast differentiation with EC50 of 1 μM. Purmorphamine can reduce both basal and induced autophagy.

L-Ascorbic Acid (Vitamin C)

Vitamin C (L-Ascorbic Acid) is a water-soluble Vitamin indicated for the prevention and treatment of scurvy.

Shield-1 (Shld1)

Shield-1 is a specific, cell-permeant and high-affinity ligand of FK506-binding protein-12 (FKBP). Shield-1 reverses the instability by binding to mutated FKBP (mtFKBP), allowing conditional expression of mtFKBP-fused proteins. Shield-1 stabilises the entire fusion protein.

Triptolide

Triptolide is a diterpene triepoxide, an immunosuppressive agent extracted from the Chinese herb Tripterygium wilfordii. It functions as a NF-κB inhibitor with dual actions by disruption of p65/CBP interaction and by reduction of p65 protein. Triptolide (PG490) abrogates the transactivation function of heat shock transcription factor 1 (HSF1). Triptolide inhibits MDM2 and induces apoptosis through a p53-independent pathway.

Tauroursodeoxycholic Acid (TUDCA)

Tauroursodeoxycholic Acid (TUDCA) is the taurine conjugate of ursodeoxycholic acid (UDCA) and acts as a mitochondrial stabilizer and anti-apoptotic agent in several models of neurodegenerative diseases, including AD, Parkinson's diseases (PD), and Huntington's diseases (HD).

N-Ethylmaleimide (NEM)

NEM (N-Ethylmaleimide) is an organic compound that is derived from maleic acid. It is an irreversible inhibitor of all cysteine peptidases, with alkylation occurring at the active site thiol group. N-Ethylmaleimide (NEM) inactivates endogenous deubiquitinating enzymes (DUBs). N-Ethylmaleimide (NEM) specifically inhibits phosphate transport in mitochondria.

Isoquercitrin

Isoquercitrin (Hirsutrin, 3-Glucosylquercetin, Quercetin 3-o-glucopyranoside), a flavonoid compound with anticancer activity isolated from Bidens bipinnata L, is an inhibitor of Wnt/ A-catenin that acts downstream of the A-catenin nuclear translocation.

Deferiprone

Deferiprone (CP20) is a chelating agent with an affinity for ferric ion (iron III), binds with ferric ions to form neutral 3:1 (Deferiprone:iron) complexes that are stable over a wide range of pH values.

Ticagrelor

Ticagrelor (AZD6140, AR-C 126532XX) is the first reversibly binding oral P2Y12 receptor antagonist with K_i of 2 nM.

Fidaxomicin

Fidaxomicin is a narrow spectrum macrocyclic antibiotic that inhibits RNA polymerase sigma subunit.

HCQ (Hydroxychloroquine) Sulfate

Hydroxychloroquine (HCQ) Sulfate is an antimalarial agent used for the treatment of systemic lupus erythematosus, rheumatoid arthritis and other autoimmune, inflammatory and dermatologic conditions. Also acts as an inhibitor of Autophagy and toll-like receptor (TLR) 7/9.

iGOT1-01

iGOT1-01, a potent aspartate aminotransferase 1 (glutamate oxaloacetate transaminase 1; GOT1) inhibitor, possesses anti-cancer activity.

Palbociclib (PD-0332991)

Palbociclib (PD 0332991) is a highly specific inhibitor of cyclin-dependent kinase 4 (Cdk4) and Cdk6 with IC50 of 11 nM and 16 nM, respectively. This product has poor solubility; animal in vivo experiments are available, cell experiments please choose carefully!

SBE-β-CD

SBE-β-CD is a novel, chemically modified cyclodextrin with a structure designed to optimize the solubility and stability of drugs.

2-DG (2-Deoxy-D-glucose)

2-DG (2-Deoxy-D-glucose), an analog of glucose, is a glycolytic inhibitor with antiviral activity. 2-Deoxy-D-glucose induces apoptosis and inhibits Herpes Simplex Virus type-1 (HSV-1) receptor expression.

JNK-IN-8

JNK-IN-8 (JNK Inhibitor XVI) is the first irreversible JNK inhibitor for JNK1, JNK2 and JNK3 with IC50 of 4.7 nM, 18.7 nM and 1 nM, >10-fold selectivity against MNK2, Fms and no inhibition to c-Kit, Met, PDGFRβin A375 cell line.

SN-38

SN-38 (NK012) is an active metabolite of CPT-11, inhibits DNA topoisomerase I, DNA synthesis and causes frequent DNA single-strand breaks. SN-38 induces autophagy.

Rucaparib (AG-014699)

Rucaparib is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains.

CP-690550 (Tofacitinib) Citrate

Tofacitinib citrate (CP-690550, Tasocitinib) is a novel JAK inhibitor with IC50 of 1 nM, 20 nM and 112 nM against JAK3, JAK2, and JAK1, respectively. It also has Anti-infection activity.

FTY720 (Fingolimod) Hydrochloride

Fingolimod (FTY720, Fingolimod Hydrochloride) HCl is a S1P antagonist with IC50 of 0.033 nM in K562, and NK cells. Please use saline solution rather than PBS for dilutions. PBS may cause precipitation.

FK506 (Tacrolimus)

Tacrolimus (FK506) is a 23-membered macrolide lactone; it reduces peptidyl-prolyl isomerase activity in T cells by binding to the immunophilin FKBP12 (FK506 binding protein), creating a new complex. Tacrolimus also inhibits the phosphatase activity of calcineurin. Tacrolimus induces vascular endothelial autophagy.

Methotrexate disodium

Methotrexate sodium, an analog of folic acid, is a nonspecific inhibitor of the dihydrofolate reductase(DHFR) of bacteria and cancerous cells as well as normal cells. It forms an inactive ternary complex with DHFR and NADPH. Methotrexate (MTX) induces apoptosis.

Doxycycline

Doxycycline (Vibramycin, Doxytetracycline, Doxiciclina, Doxycyclinum) is an antibiotic that is used in the treatment of a number of types of infections caused by bacteria and protozoa. Doxycycline is also a nonspecific matrix metalloproteinase (MMP) inhibitor.

Ribociclib hydrochloride

Ribociclib (LEE011) hydrochloride is a highly specific dual inhibitor of CDK4 and CDK6 with IC50 of 10 nM and 39 nM, respectively.

Ruxolitinib (INCB18424) Phosphate

Ruxolitinib Phosphate (INCB018424, INC424) is the phosphate salt form of Ruxolitinib. Ruxolitinib is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM in cell-free assays, >130-fold selectivity for JAK1/2 versus JAK3. Ruxolitinib kills tumour cells through toxic mitophagy. Ruxolitinib induces autophagy and enhances apoptosis.

Dasatinib hydrochloride

Dasatinib hydrochloride (BMS-354825) is the hydrochloride salt form of dasatinib, an inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM in cell-free assays, respectively.

β-nicotinamide mononucleotide (NMN)

Nicotinamide mononucleotide (β-NM, NMN), one of the key precursors of NAD+ and products of the NAMPT reaction, is converted to NAD+ by nicotinamide mononucleotide adenylyltransferase.

RU58841

RU58841, also known as PSK-3841 or HMR-3841, is a non-steroidal anti-androgen.

Abemaciclib (LY2835219)

Abemaciclib is a Cell Cycle inhibitor selective for CDK4/6 with IC50 of 2 nM and 10 nM in cell-free assays, respectively.

Deferoxamine mesylate

Deferoxamine mesylate is the mesylate salt of Deferoxamine, which forms iron complexes and is used as a chelating agent. Deferoxamine is a ferroptosis inhibitor that stabilises HIF-1α expression and improves HIF-1α transactivity in hypoxic and hyperglycaemic states in vitro. Deferoxamine decreases beta-amyloid (Aβ) deposition and induces autophagy.Please do not prepare stock solutions with normal saline or PBS, as precipitation may occur.

Relugolix (TAK-385, RVT-601)

Relugolix (RVT-601, TAK-385) is a selective antagonist of the gonadotropin-releasing hormone receptor (GnRHR) with IC50 of 0.33 nM and 0.32 nM for human GnRHR and monkey GnRHR, respectively.

Larotrectinib (LOXO-101)

Larotrectinib (Vitrakvi, LOXO-101, ARRY-470) is an ATP-competitive, orally administered and highly selective inhibitor of the tropomyosin-related kinase (TRK) family receptors.

Heparan Sulfate

Heparan sulfate (HS, Heparitin sulfate, Alpha-idosane, HHS 5, N-Acetylheparan Sulfate, Suleparoid, Tavidan), a constituent of HS proteoglycans (HSPGs), is a linear polysaccharide present on the cell surface. Heparan sulfate influences the binding affinity of intestinal epithelium cells (IECs) to Wnt, thereby promoting activation of canonical Wnt signaling and facilitating regeneration of small intestinal crypts after epithelial injury.

Guanidinoacetic acid

Guanidinoacetic acid (Guanidino acetic acid, GAA, Glycocyamine, Guanidinoacetate), the natural precursor of creatine, is under investigation as a dietary agent. Guanidinoacetic acid exhibits potential ergogenic benefits for physically active men and women.

Y-27632

Y-27632 is a selective ROCK1 and ROCK2 inhibitor with a Ki of 140 nM and 300nM in a cell-free assay, exhibits >200-fold selectivity over other kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK.

Mitapivat (AG-348)

Mitapivat (AG-348) is an activator of a pyruvate kinase PKM2, an enzyme involved in glycolysis.

AZD5069

AZD5069 is a novel antagonist of CXCR2, which is shown to inhibit binding of CXCL8 to CXCR2 with a pIC50 value of 8.8 and inhibit CXCL8 binding to CXCR1 with pIC50 values of 6.5.

H-151

H-151 is a highly potent and covalent inhibitor of STING that has noteworthy inhibitory activity both in human cells and in vivo.

SRI-011381 (C381)

SRI-011381 (C381) is a novel agonist of the TGF-beta signaling pathway for treatment of Alzheimer's disease. C381 physically targets the lysosome, promotes lysosomal acidification, increases breakdown of lysosomal cargo, and improves lysosome resilience to damage.

(R)-GNE-140

(R)-GNE-140 is an inhibitory agent for LDHA, LDHB, and LDHC, with IC50 values of 3 nM and 5 nM for LDHA and LDHB, respectively. (R)-GNE-140 is 18 times more potent than its S isomer.

Bobcat339 Hydrochloride

Bobcat339 is a selective cytosine-based TET enzyme inhibitor with IC50 of 33 μM and 73 μM for TET1 and TET2, respectively. Bobcat339 can reduce DNA 5-hydroxymethylcytosine abundance by inhibiting TET enzyme function in living cells and provide support for its utility as a viable pharmacological probe.

Corn Oil

Corn Oil is a refined vegetable oil used as a delivery vehicle for fat-soluble compounds, including toxins. It is also used in the delivery of tamoxifen (TAM) in mice, curcumin in rats, and [3H]retinol in mice.

Tween 80

Tween 80 is a polysorbate surfactant used for selective protein extraction and the isolation of nuclei from mammalian cell lines. Tween 80 has been used in drug vehicle solutions for specific injections in mice and rats. It has been used for the determination of esterase activity in bacterial cells.

CMC-Na

CMC-Na (Sodium carboxymethyl cellulose) is one of the important modified cellulose, a water-soluble cellulose, which is widely used in many application of food, pharmaceuticals, detergent, paper coating, dispersing agent, and Others. Its addition possibly increases the hydrogenation and dehydrogenation features of Magnesium.

PEG300

PEG300 (Polyethylene glycol 300) is a water-miscible polyether widely used in biochemistry, structural biology, and medicine in addition to pharmaceutical and chemical industries. It serves as a kind of solubiliser, excipient, lubricant, and chemical reagent. PEG300 helps in the formation of hydrogels in situ upon mixing with silk. These PEG–silk hydrogels are of interest for many biomedical applications, such as anti-fouling and anti-adhesion.

PEG400

PEG400b (Polyethylene glycol 400) is a commonly used co-solvent used in a variety of pharmaceutical formulations. It acts as a good solubiliser and surfactant and has the potential to improve the bioavailability of drugs. PEG400 significantly accelerates the metabolism of baicalein and increases the penetration of BG and B6G in Caco-2 cells.

Darovasertib (LXS196)

Darovasertib (LXS-196, IDE-196) is a selective inhibitor of protein kinase C (PKC).

Sodium oxamate

Sodium oxamate (SO, Aminooxoacetic acid, Oxamic acid) is an inhibitor of lactate dehydrogenase (LDH) that specifically inhibits LDH‑A. Sodium oxamate (SO) induces G2/M cell cycle arrest via downregulation of the CDK1/cyclin B1 pathway and promotes apoptosis through enhancement of mitochondrial ROS generation.

Clozapine N-oxide (CNO chemical)

CNO (Clozapine N-oxide) is a metabolite of Clozapine (GLXC-06516) and an agonist of human muscarinic designer receptors (Designer Receptors Exclusively Activated by Designer Drugs, DREADDs). Clozapine is a potent dopamine (DA) antagonist and a selective muscarinic M4 receptor agonist.Solutions are unstable and should be fresh-prepared.

S961

S961 is a biosynthetic insulin receptor antagonist that inhibits cellular proliferation and colony formation in breast tumour cells.

Bavdegalutamide (ARV-110)

Bavdegalutamide (ARV-110) is an orally bioavailable, specific androgen receptor (AR) PROTAC degrader that leads to ubiquitination and degradation of AR. ARV-110 completely degrades androgen receptor (AR) in all cell lines tested with DC50 of < 1 nM. ARV-110 can be used for the research of prostate cancer.

Ervogastat (PF-06865571)

Ervogastat (PF-06865571, DGAT2i) is a potent diacylglycerol acyltransferase 2 (DGAT2) inhibitor that reduces steatosis and hepatic triglyceride levels in non-alcoholic steatohepatitis (NASH).

Guadecitabine sodium

Guadecitabine sodium (SGI-110 sodium; S-110 sodium) is a next-generation hypomethylating agent.

Z-VAD-FMK

Z-VAD-FMK (Z-VAD(OMe)-FMK) is a cell-permeable, irreversible pan-caspase inhibitor, blocks all features of apoptosis in THP.1 and Jurkat T-cells.

IPI-145 (Duvelisib)

Duvelisib (IPI-145, INK1197) is a novel and selective PI3K δ/γ inhibitor with K_i and IC50 of 23 pM/243 pM and 1 nM/50 nM in cell-free assays, highly selective for PI3K δ/γ than other protein kinases. Phase 3.

RG-7112

RG7112 (RO5045337) is an orally bioavailable and selective p53-MDM2 inhibitor with HTRF IC50 of 18 nM.

Wnt-C59 (C59)

Wnt-C59 (C59) is a PORCN inhibitor for Wnt3A-mediated activation of a multimerised TCF-binding site driving luciferase with IC50 of 74 pM in HEK293 cells.

BMN-673 (Talazoparib)

Talazoparib (BMN 673, LT-673) is a novel PARP inhibitor with IC50 of 0.57 nM for PARP1 in a cell-free assay. It is also a potent inhibitor of PARP-2, but does not inhibit PARG and is highly sensitive to PTEN mutation. Phase 3.

Tezacaftor (VX-661)

Tezacaftor (VX-661) is a second F508del CFTR corrector and is believed to help CFTR protein reach the cell surface. Phase 2.

GSK126

GSK126 (GSK2816126A, GSK2816126) is a potent, highly selective EZH2 methyltransferase inhibitor with IC50 of 9.9 nM, >1000-fold selective for EZH2 over 20 other human methyltransferases.

Pinometostat (EPZ5676)

Pinometostat (EPZ5676) is an S-adenosyl methionine (SAM) competitive inhibitor of protein methyltransferase DOT1L with K_i of 80 pM in a cell-free assay, demonstrating >37,000-fold selectivity against all other PMTs tested, inhibits H3K79 methylation in tumour. Phase 1.

Tepotinib (EMD-1214063)

Tepotinib is a potent and selective c-Met inhibitor with IC50 of 4 nM, >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer. Tepotinib (EMD 1214063) induces autophagy. Phase 1.

GSK-J4 Hydrochloride

GSK J4 HCl is a cell permeable prodrug of GSK J1, which is the first selective inhibitor of the H3K27 histone demethylase JMJD3 and UTX with IC50 of 60 nM in a cell-free assay and inactive against a panel of demethylases of the JMJ family.

IWP-2

IWP-2 is an inhibitor of Wnt processing and secretion with IC50 of 27 nM in a cell-free assay, selective blockage of Porcn-mediated Wnt palmitoylation, does not affect Wnt/β-catenin in general and displays no effect against Wnt-stimulated cellular responses. IWP-2 specifically inhibits CK1δ.

IWR-1-endo

IWR-1-endo (endo-IWR 1, IWR-1) is a Wnt pathway inhibitor with an IC50 of 180 nM in L-cells expressing Wnt3A, it induces Axin2 protein levels and promotes β-catenin phosphorylation by stabilising Axin-scaffolded destruction complexes.

SM-164

SM-164 is a potent, non-peptide, cell-permeable antagonist of XIAP that targets both the BIR2 and BIR3 domains with IC50 of 1.39 nM. SM-164 induces apoptosis and tumour regression.

(-)-Blebbistatin

(-)-Blebbistatin ((S)-(-)-Blebbistatin) is a cell-permeable inhibitor for non muscle myosin II ATPase with IC50 of ~2 μM in cell-free assays, does not inhibit myosin light chain kinase, inhibits contraction of the cleavage furrow without disrupting mitosis or contractile ring assembly.

SCH772984

SCH772984 is a novel, specific inhibitor of ERK1/2 with IC50 values of 4 nM and 1 nM in cell-free assay, respectively, And show robust efficacy in RAS- or BRAF-mutant cancer cells.

Berzosertib (VE-822)

Berzosertib (VE-822, VX970, M6620) is an ATR inhibitor with an IC50 of 19 nM in HT29 cells.

MLN4924 (Pevonedistat)

MLN4924 is a small molecule inhibitor of Nedd8 activating enzyme (NAE) with IC50 of 4 nM.

(+)-JQ1

(+)-JQ1 is a BET bromodomain inhibitor, with IC50 of 77 nM/33 nM for BRD4(1/2) in cell-free assays, binding to all bromodomains of the BET family, but not to bromodomains outside the BET family. (+)-JQ1 suppresses cell proliferation via inducing autophagy. (+)-JQ1 inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes.

3-Deazaneplanocin A (DZNep) Hydrochloride

DZNeP (3-deazaneplanocin A) HCl, an analog of adenosine, is a competitive inhibitor of S-adenosylhomocysteine hydrolase with K_i of 50 pM in a cell-free assay.

EPZ-6438 (Tazemetostat)

Tazemetostat (EPZ-6438, E7438) is a potent, and selective EZH2 inhibitor with K_i and IC50 of 2.5 nM and 11 nM in cell-free assays, exhibiting a 35-fold selectivity versus EZH1 and >4,500-fold selectivity relative to 14 other HMTs.

LGK974 (WNT974)

LGK-974 (NVP-LGK974, WNT974) is a potent and specific PORCN inhibitor, and inhibits Wnt signalling with IC50 of 0.4 nM in TM3 cells. Phase 1.

Marimastat (BB-2516)

Marimastat (BB-2516, TA2516) is a broad spectrum matrix metalloprotease (MMP) inhibitor for MMP-9, MMP-1, MMP-2, MMP-14 and MMP-7 with IC50 of 3 nM, 5 nM, 6 nM, 9 nM and 13 nM, respectively. Phase 3.

Ilomastat (GM6001)

Ilomastat (GM6001) is a broad spectrum matrix metalloprotease (MMP) inhibitor for MMP-1, MMP-2, MMP-3, MMP-7, MMP-8, MMP-9, MMP-12, MMP-14, and MMP-26 with K_i of 0.4 nM, 0.5 nM, 27 nM, 3.7 nM, 0.1 nM, 0.2 nM, 3.6 nM, 13.4 nM, and 0.36 nM, respectively.

LY2835219 (Abemaciclib) Mesylate

Abemaciclib mesylate is a potent and selective inhibitor of CDK4 and CDK6 with IC50 of 2 nM and 10 nM in cell-free assays, respectively. Phase 3.

Avutometinib (Ro5126766, CH5126766)

Avutometinib(RO5126766,CH5126766,VS 6766, CKI-27, R-7304, RG-7304) is a dual RAF/MEK inhibitor with IC50 of 8.2 nM, 19 nM, 56 nM, and 160 nM for BRAF V600E, BRAF, CRAF, and MEK1, respectively. Phase 1.

Setanaxib (GKT137831)

Setanaxib (GKT137831, GKT831) is a potent, dual NADPH oxidase NOX1/NOX4 inhibitor with Ki of 110 nM and 140 nM, respectively. Treatment with GKT137831 suppresses reactive oxygen species (ROS) production. GKT137831 partly inhibits ferroptosis.

Opaganib (ABC294640)

Opaganib (ABC294640) is an orally bioavailable and selective sphingosine kinase-2 (SphK2) inhibitor with IC50 of approximately 60 μM. Phase 1/2.

Prexasertib (LY2606368) Dihydrochloride

Prexasertib (LY2606368) is an ATP-competitive CHK1 inhibitor with a Ki value of 0.9 nmol/L. For CHK2 and RSK, its IC50 values are 8 nM and 9 nM respectively in cell-free assay.

Molibresib (I-BET-762)

Molibresib (I-BET-762, GSK525762, GSK525762A) is an inhibitor for BET proteins with IC50 of ~35 nM in a cell-free assay, suppresses the production of proinflammatory proteins by macrophages and blocks acute inflammation, highly selective over other bromodomain-containing proteins.

PF-04418948

PF-04418948 is a potent and selective prostaglandin EP₂ receptor antagonist with IC50 of 16 nM. Phase 1.

RepSox (E-616452)

RepSox (E-616452, SJN 2511, ALK5 Inhibitor II) is a potent and selective inhibitor of TGFβR-1/ALK5 with an IC50 of 23 nM and 4 nM for ATP binding to ALK5 and ALK5 autophosphorylation in cell-free assays, respectively.

RGFP966

RGFP966 is an HDAC3 inhibitor with an IC50 of 0.08 μM in a cell-free assay, exhibiting > 200-fold selectivity over other HDAC.

Erastin

Erastin is a ferroptosis activator by acting on mitochondrial VDAC, exhibiting selectivity for tumour cells bearing oncogenic RAS. Solutions are unstable and should be fresh-prepared.

Ferrostatin-1 (Fer-1)

Fer-1 (Ferrostatin-1) is a potent and selective inhibitor of ferroptosis with an EC50 of 60 nM.

Selinexor (KPT-330)

Selinexor (KPT-330, ATG-010) is an orally bioavailable selective CRM1 inhibitor. Phase 2.

AZD9291 (Osimertinib)

Osimertinib (AZD9291) is an oral, irreversible, and mutant-selective EGFR inhibitor with IC50 of 12.92, 11.44 and 493.8 nM for Exon 19 deletion EGFR, L858R/T790M EGFR, and WT EGFR in LoVo cells, respectively. Phase 3.

Dorsomorphin Dihydrochloride

Dorsomorphin 2HCl is a potent, reversible, selective AMPK inhibitor with K_i of 109 nM in cell-free assays, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. Also inhibits type Ⅰ BMP receptor activity. Dorsomorphin induces autophagy in cancer cell line.

Q-VD-Oph

Q-VD-Oph (Quinoline-Val-Asp-Difluorophenoxymethylketone) is a potent pan-caspase inhibitor with IC50 ranged from 25 to 400 nM for caspases 1,3,8, and 9. Q-VD-OPh can inhibit HIV infection.

Z-DEVD-FMK

Z-DEVD-FMK (Caspase-3 Inhibitor) is a specific, irreversible Caspase-3 inhibitor, and also shows potent inhibition on caspase-6, caspase-7, caspase-8, and caspase-10.

Calpeptin

Calpeptin is a potent, cell-permeable calpain inhibitor with ID50 of 52 nM, 34 nM, 138 nM, and 40 nM for Calpain I (porcine erythrocytes), Calpain II (porcine kidney), Papainb, and Calpain I (human platelets), respectively. Calpeptin attenuates apoptosis and intracellular inflammatory changes in muscle cells.

Sorafenib (BAY 43-9006)

Sorafenib is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity.

Cycloheximide

Cycloheximide, an antifungal antibiotic, is a eukaryote protein synthesis inhibitor with IC50 of 532.5 nM and 2880 nM for protein synthesis and RNA synthesis in vivo, respectively. Cycloheximide suppresses ferroptosis and inhibits autophagy.Cycloheximide (NSC-185) can be used to induce animal models of Dysmnesia.Solutions are unstable and should be fresh-prepared.This product is a hazardous chemical (acute toxicity/flammable/skin corrosive). Please use it while wearing a protective face mask, gloves, and clothing.

LEE011 (Ribociclib)

Ribociclib is an orally available, and highly specific inhibitor of CDK4 and CDK6 with IC50 of 10 nM and 39 nM. Phase 3.

AP-III-a4 (ENOblock)

AP-III-a4 (ENOblock) is the first nonsubstrate analogue inhibitor of enolase with IC50 of 0.576 μM.

FTI 277 HCl

FTI 277 HCl is a potent and selective farnesyltransferase (FTase) inhibitor with IC50 of 500 pM, about 100-fold selectivity over the closely related GGTase I. FTI 277 HCl inhibits cell growth and induces apoptosis. FTI 277 HCl is effective in clearing HDV viremia.

LDN-193189 Dihydrochloride

LDN-193189 (DM3189) 2HCl is a selective BMP signaling inhibitor, inhibits the ALK1, ALK2, ALK3 and ALK6 with IC50s of 0.8 nM, 0.8 nM, 5.3 nM and 16.7 nM in the kinase assay, respectively. LDN-193189 inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50s of 5 nM and 30 nM in C2C12 cells, respectively, exhibits 200-fold selectivity for BMP versus TGF-β.

Darapladib (SB-480848)

Darapladib is a reversible lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor with IC50 of 0.25 nM. Phase 3.

Vactosertib (TEW-7197)

Vactosertib (TEW-7197, EW-7197) is a highly potent, selective, and orally bioavailable TGF-β receptor ALK4/ALK5 inhibitor with IC50 of 13 nM and 11 nM, respectively. Phase 1.

SB273005

SB273005 is a potent integrin inhibitor with K_i of 1.2 nM and 0.3 nM for αvβ3 receptor and αvβ5 receptor, respectively.

Ravoxertinib (GDC-0994)

Ravoxertinib (GDC-0994) is a potent, orally available and highly selective ERK1/2 inhibitor with IC50 of 1.1 nM and 0.3 nM, respectively. Phase 1.

ODM-201 (Darolutamide)

Darolutamide (ODM-201, BAY-1841788) is a novel Androgen Receptor (AR) antagonist that blocks AR nuclear translocation with K_i of 11 nM. Phase 3.

WH-4-023

WH-4-023 (KIN001-112, KIN112, Dual LCK/SRC inhibitor) is a potent and orally active Lck/Src inhibitor with IC50s of 2 nM and 6 nM in cell-free assays, respectively. Exhibits >300-fold selectivity against p38α and KDR. Also potently inhibits SIK (IC50 values are 10, 22 and 60 nM for SIK 1, 2 and 3 respectively) and displays selectivity over a range of closely related kinases.

Leptomycin B (LMB)

Leptomycin B (LMB, CI 940, Elactocin, Mantuamycin, NSC 364372) is a potent antifungal antibiotic isolated from Streptomyces and acts as a specific inhibitor of the nuclear export factor CRM1. Leptomycin B rapidly induces cytotoxic effects in cancer cell lines via covalent inhibition of CRM1 with IC50 values of 0.1 nM–10 nM.

BV6

BV-6 is a SMAC mimetic, dual cIAP and XIAP inhibitor.

SB 225002

SB225002 is a potent and selective CXCR2 antagonist with an IC50 of 22 nM for inhibiting interleukin IL-8 binding to CXCR2, > 150-fold selectivity over the other 7-TMRs tested.

Defactinib (VS-6063)

Defactinib (VS-6063, PF-04554878) is a selective, and orally active FAK inhibitor. Phase 2.

Telaglenastat (CB-839)

Telaglenastat (CB-839) is a potent, selective, and orally bioavailable glutaminase inhibitor with IC50 of 24 nM for recombinant human GAC. CB-839 (Telaglenastat) induces autophagy and has antitumor activity. Phase 1.

SU 5402

SU5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC50 of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGF-Rβ, respectively.

Omaveloxolone (RTA-408)

Omaveloxolone (RTA-408) is a synthetic triterpenoid that activates the cytoprotective transcription factor Nrf2 and inhibits NF-κB signaling. Phase 2.

SAR405

SAR405 is a low-molecular-mass kinase inhibitor of PIK3C3/Vps34 (KD 1.5 nM) showing high selectivity and not be active up to 10 μM on class I and class II PI3Ks as well as on mTOR. SAR405 prevents autophagy and synergizes with MTOR (mechanistic target of rapamycin) inhibition in tumour cells.

A-83-01

A-83-01 is a potent inhibitor of TGF-β type I receptor (ALK5-TD) with an IC50 of 12 nM. A-83-01 also inhibits the transcription induced by activin/nodal type I receptor (ALK4-TD) and nodal type I receptor (ALK7-TD) with IC50 values of 45 nM and 7.5 nM, respectively.Solutions are unstable and should be fresh-prepared.

Ceralasertib (AZD6738)

Ceralasertib (AZD6738) is an orally active, and selective ATR kinase inhibitor with IC50 of 1 nM. Phase 1/2.

Liproxstatin-1

Liproxstatin-1 is a potent ferroptosis inhibitor with an IC50 of 22 nM.

A-438079 Hydrochloride

A-438079 HCl is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9.

MMAE (Monomethyl auristatin E)

MMAE (Monomethyl auristatin E) is a synthetic antineoplastic agent. It is also a microtubule-disrupting agent.

Eprenetapopt (APR-246)

Eprenetapopt (APR-246, PRIMA-1MET) is a small organic molecule that has been shown to restore tumour-suppressor function primarily to mutant p53 and also to induce cell death in various cancer types. APR-246 induces Apoptosis and Autophagy.

Sotuletinib (BLZ945)

Sotuletinib (BLZ945) is an orally active, potent and selective CSF-1R inhibitor with an IC50 of 1 nM, >1000-fold selective against its closest receptor tyrosine kinase homologs.

Ro-3306

RO-3306 is an ATP-competitive, and selective CDK1 inhibitor with K_i of 20 nM, >15-fold selectivity against a diverse panel of human kinases. RO-3306 enhances p53-mediated Bax activation and mitochondrial apoptosis.

ASP2215 (Gilteritinib)

Gilteritinib (ASP2215) is a small-molecule FLT3/AXL inhibitor with IC50 values of 0.29 nM and 0.73 nM for FLT3 and AXL, respectively. It inhibits FLT3 at an IC50 value that was approximately 800-fold more potent than the concentration required to inhibit c-KIT (230 nM).

GSK1265744 (Cabotegravir)

Cabotegravir (GSK744, GSK1265744, S/GSK1265744) is a long-acting HIV integrase inhibitor against a broad range of HIV subtypes, and inhibits the HIV-1 integrase catalysed strand transfer reaction with IC50 of 3.0 nM. Phase 2.

Emricasan (IDN-6556)

Emricasan (IDN-6556, PF 03491390, PF-03491390) is a potent irreversible pan-caspase inhibitor. Emricasan is an inhibitor of Zika virus infection.

SAG (Smoothened Agonist) Hydrochloride

SAG (Smoothened Agonist) HCl is a cell-permeable Smoothened (Smo) agonist with EC50 of 3 nM in Shh-LIGHT2 cells.

Erlotinib (CP-358774)

Erlotinib is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl. Erlotinib induces autophagy.

PMA chemical (Phorbol 12-myristate 13-acetate)

PMA (Phorbol 12-myristate 13-acetate), a potent activator of PKC, is active at nanomolar concentrations. Phorbol 12-myristate 13-acetate (PMA) induces sphingosine-1-phosphate (S1P). PMA has strong excitability on the skin and mucous membrane. Special protection is required when using PMA. Wear gloves and a mask to avoid direct contact in any way.

Gsk484 Hydrochloride

GSK484 HCl, a benzoimidazole derivative, is a selective and reversible inhibitor of peptidylarginine deiminase 4 (PAD4) with IC50 of 50 nM in the absence of Calcium.

MCC950 Sodium

MCC950 Sodium is a potent, selective inhibitor of NLRP3 with IC50 of 7.5 nM in BMDMs; but not the AIM2, NLRC4 or NLRP1 inflammasomes.

Pexidartinib (PLX3397)

Pexidartinib (PLX3397) is an oral, potent multi-targeted receptor tyrosine kinase inhibitor of CSF-1R, Kit (c-Kit), and FLT3 with IC50 of 20 nM, 10 nM and 160 nM, respectively. Pexidartinib (PLX3397) induces apoptosis and necrosis with antitumor activity. Phase 3.

4-Hydroxytamoxifen (Afimoxifene)

4-Hydroxytamoxifen (Afimoxifene) is the active metabolite of tamoxifen and a selective estrogen receptor (ER) modulator that is widely used in the therapeutic and chemopreventive treatment of breast cancer. It activates on-target modification frequency for intein-Cas9 variants.

LY3009120

LY03009120 (DP-4978) is a potent pan-Raf inhibitor with IC50 of 44 nM, 31-47 nM, and 42 nM for A-raf, B-Raf, and C-Raf in A375 cells, respectively. LY03009120 induces autophagy. Phase 1.

Pelabresib (CPI-0610)

Pelabresib (CPI-0610) is a potent and selective benzoisoxazoloazepine BET bromodomain inhibitor with an IC50 of 39 nM for BRD4-BD1 in TR-FRET assay and currently undergoing human clinical trials for haematological malignancies. CPI-0610 inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes.

Ulixertinib (BVD-523)

Ulixertinib (BVD-523, VRT752271) is a potent and reversible ERK1/ERK2 inhibitor with IC50 of <0.3 nM for ERK2. Phase 1.

8-Bromo-cAMP (8-Br-cAMP) Sodium Salt

8-Bromo-cAMP sodium salt is a cell permeable analog of cAMP that activates cyclic-AMP-dependent protein kinase with a Ka value of 0.05 μM; and a PKA activator.

Dibutyryl cAMP (db cAMP/Bucladesine) sodium

Bucladesine sodium is a cell-permeable PKA activator by mimicking the action of endogenous cAMP. Dibutyryl-cAMP (Bucladesine) is also a phosphodiesterase (PDE) inhibitor.

SC79

SC79 is a brain-penetrable Akt phosphorylation activator and an inhibitor of Akt-PH domain translocation.

740 Y-P (PDGFR 740Y-P)

740 Y-P (PDGFR 740Y-P, 740YPDGFR) is a cell-permeable phosphopeptide activator of PI3K.

Disodium (R)-2-Hydroxyglutarate

Disodium (R)-2-Hydroxyglutarate (D-α-Hydroxyglutaric acid disodium) is a competitive inhibitor of α-ketoglutarate-dependent dioxygenases with K_i of 10.87 ± 1.85 mM.

Concanamycin A

Concanamycin A (Folimycin; Antibiotic X 4357B) is a macrolide antibiotic, a vacuolar type H+-ATPase (V-ATPase) inhibitor. Concanamycin A is also an inhibitor of lysosomal acidification, can be used to T cell-mediated inflammation research-.

Tunicamycin

Tunicamycin, an Antibiotic, can potently inhibit the N-linked glycosylation (NLG) by competitively inhibiting UDP-GlcNAc-dolichol-phosphate N-acetylglucosamine-1 phosphate transferase (DPAGT1) activity and can target several types of tumours by reducing angiogenesis, inhibiting colony formation, and enhancing TRAIL-induced apoptosis.

Thapsigargin

Thapsigargin is a potent, non-competitive inhibitor of the sarco/endoplasmic reticulum Ca²⁺ ATPase (SERCA) with IC50 of 0.353 nM or 0.448 nM for the carbachol-evoked [Ca2+]i-transients with or without a KCl-prestimulation. Thapsigargin induces cell apoptosis. Thapsigargin is extracted from a plant, Thapsia garganica.

ISX-9 (Isoxazole 9)

ISX-9 (Isoxazole 9) is a synthetic promoter of adult neurogenesis by triggering neuronal differentiation of adult neural stem/precursor cells (NSPCs). ISX-9 (Isoxazole 9) activates multiple pathways including TGF-β induced epithelial–mesenchymal transition (EMT) signalling, canonical and non-canonical Wnt signalling at different stages of cardiac differentiation.

Bay K 8644

Bay K 8644 is a racemate. Bay K 8644 is a potent, selective activator of L-type Ca2+ channel with an IC50 of 17.3 nM.

KD025 (Belumosudil)

Belumosudil (KD025, SLx-2119) is an orally available, and selective ROCK2 inhibitor with IC50 and K_i of 60 nM and 41 nM, respectively. Phase 2.

SIS3 Hydrochloride

SIS3, a novel specific inhibitor of Smad3, inhibits TGF-β and activin signalling by suppressing Smad3 phosphorylation without affecting the MAPK/p38, ERK, or PI3-kinase signalling pathways.

Napabucasin (BBI608)

Napabucasin (BBI608) is an orally available Stat3 and cancer cell stemness inhibitor.

Ripasudil hydrochloride dihydrate

Ripasudil hydrochloride dihydrate is a potent ROCK inhibitor with IC50 of 51 nM and 19 nM for ROCK1 and ROCK2, respectively, used for the treatment of glaucoma and ocular hypertension.

Entrectinib (Rxdx-101)

Entrectinib is an orally bioavailable pan-TrkA/B/C, ROS1 and ALK inhibitor with IC50 ranging between 0.1 and 1.7 nM. Entrectinib (RXDX-101) induces autophagy. Phase 2.

Nirogacestat (PF-03084014)

Nirogacestat (PF-03084014, PF-3084014) is a selective gamma-secretase inhibitor with IC50 of 6.2 nM in a cell-free assay. Nirogacestat (PF-03084014, PF-3084014) induces apoptosis. Phase 2.

AZD5363 (Capivasertib)

Capivasertib (AZD5363) potently inhibits all isoforms of Akt (Akt1/Akt2/Akt3) with IC50 of 3 nM/8 nM/8 nM in cell-free assays, similar to P70S6K/PKA and lower activity towards ROCK1/2. Phase 2.

BI-10773 (Empagliflozin)

Empagliflozin is a potent and selective SGLT-2 inhibitor with IC50 of 3.1 nM, exhibits >300-fold selectivity over SGLT-1, 4, 5 and 6. Phase 3.

AMD3100 (Plerixafor)

Plerixafor (AMD3100, JM 3100, SID791) is a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM in cell-free assays, respectively. Plerixafor inhibits human immunodeficiency virus (HIV) replication.

Necrostatin-1 (Nec-1)

Necrostatin-1 (Nec-1) is a specific RIP1 (RIPK1) inhibitor and inhibits TNF-α-induced necroptosis with EC50 of 490 nM in 293T cells. Necrostatin-1 also blocks IDO and suppresses autophagy and apoptosis.

Cobimetinib (GDC-0973)

Cobimetinib (GDC-0973, RG7420) is a potent and highly selective MEK1 inhibitor with IC50 of 4.2 nM, and showing no significant inhibition when tested against a panel of more than 100 of serine-threonine and tyrosine kinases. Cobimetinib induces apoptosis. Phase 3.

GW2580

GW2580 (SC-203877) is a selective CSF-1R inhibitor for c-FMS with IC50 of 30 nM, 150- to 500-fold selective compared to b-Raf, CDK4, c-KIT, c-SRC, EGFR, ERBB2/4, ERK2, FLT-3, GSK3, ITK, JAK2 etc.

KU-0060648

KU-0060648 is a dual inhibitor of DNA-PK and PI3Kα, PI3Kβ, PI3Kδ with IC50 of 8.6 nM and 4 nM, 0.5 nM, 0.1 nM respectively, less inhibition of PI3Kγ with IC50 of 0.59 μM.

Dynasore

Dynasore is a cell-permeable, reversible non-competitive dynamin inhibitor of GTPase activity of dynamin 1/2, with IC50 of 15 μM in a cell-free assay, also inhibits the mitochondrial dynamin Drp1, with no effect against other small GTPase. Dynasore suppresses mTORC1 activity and induces autophagy. Dynasore inhibits the entry of several viruses, including herpes simplex virus (HSV).

ABT-199 (Venetoclax)

Venetoclax (ABT-199, GDC-0199) is a Bcl-2-selective inhibitor with K_i of <0.01 nM in cell-free assays, >4800-fold more selective versus Bcl-xL and Bcl-w, and no activity to Mcl-1. Venetoclax is reported to induce cell growth suppression, apoptosis, cell cycle arrest, and autophagy in triple negative breast cancer MDA-MB-231 cells. Phase 3.

Tubastatin A

Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold). Tubastatin A promotes autophagy and increases apoptosis.

Nutlin-3a

Nutlin-3a ((-)-Nutlin-3), the active enantiomer of Nutlin-3, inhibits the p53/MDM2 interaction with IC50 of 90 nM in a cell-free assay. Nutlin-3a induces autophagy and apoptosis in a p53-dependent manner.

Vorapaxar (MK-5348)

Vorapaxar (SCH 530348, MK-5348) is a potent and orally active thrombin receptor (PAR-1) antagonist with K_i of 8.1 nM.

Bardoxolone Methyl (RTA 402)

Bardoxolone Methyl (RTA 402, TP-155, NSC 713200, CDDO Methyl Ester, CDDO-Me) is an IKK inhibitor, showing potent proapoptotic and anti-inflammatory activities; Also a potent Nrf2 activator and nuclear factor-κB (NF-κB) inhibitor. Bardoxolone Methyl abrogates ferroptosis. Bardoxolone methyl induces apoptosis and autophagy in cancer cells.

Resiquimod (R-848)

Resiquimod (R-848, S28463) is an immune response modifier that acts as a potent TLR 7/TLR 8 agonist that induces the upregulation of cytokines such as TNF-α, IL-6 and IFN-α. Resiquimod reduces hepatitis C virus (HCV) infection. Phase 2.

Cl-amidine

Cl-amidine is an irreversible pan-peptidylarginine deiminase (PAD) inhibitor with IC50 values of 5.9 0.3 M, 0.8 0.3 M, 6.2 1.0 M for PAD4, PAD1 and PAD3, respectively. Cl-amidine induces apoptosis.

Mitomycin C

Mitomycin C (Ametycine) is an antineoplastic antibiotic by inhibiting DNA synthesis, used to treat different cancers. Mitomycin C induces apoptosis in a caspases-dependent and Fas/CD95-independent manner.This product is a hazardous chemical (acute toxicity/flammable/skin corrosive). Please use it while wearing a protective face mask, gloves, and clothing.

RSL3

RSL3 ((1S,3R)-RSL3) is a ferroptosis activator in a VDAC-independent manner, exhibiting selectivity for tumour cells bearing oncogenic RAS. RSL3 binds, inactivates GPX4 and thus mediates GPX4-regulated ferroptosis.

ON123300

ON123300 is a potent and multi-targeted kinase inhibitor with IC50 of 3.9 nM, 5 nM, 26 nM, 26 nM, 9.2 nM and 11nM for CDK4, Ark5/NUAK1, PDGFRβ, FGFR1, RET (c-RET), and Fyn, respectively.

ABT-494 (Upadacitinib)

Upadacitinib is a selective JAK1 inhibitor which demonstrates activity against JAK1 (0.045 M) and JAK2 (0.109 M), with > 40 fold selectivity over JAK3 (2.1 M) and 100 fold selectivity over TYK2 (4.7 M) as compared to JAK1.

Paxalisib (GDC-0084)

Paxalisib (GDC-0084, RG7666) is a brain penetrant inhibitor of PI3K and mTOR with Kiapp values of 2 nM, 46 nM, 3 nM, 10 nM and 70 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR.

Ro 61-8048

Ro 61-8048 is a high-affinity kynurenine 3-hydroxylase (KMO) inhibitor with IC50 and K_i of 37 nM and 4.8 nM, respectively.

Cytochalasin D

Cytochalasin D (Zygosporin A, NSC 209835) is a potent actin polymerization inhibitor derived from fungus. Cytochalasin D inhibits actin filament dynamics in cells. It induces phosphorylation and cytoplasmic retention of Yap.

AG-221 (Enasidenib)

Enasidenib (AG-221) is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzyme.

Netarsudil (AR-13324) 2HCl

Netarsudil (AR-13324) is a ROCK inhibitor with Ki value of 0.2-10.3 nM. It is currently in clinical trials for the treatment of glaucoma and ocular hypertension.

Etomoxir sodium salt

Etomoxir sodium salt ((R)-(+)-Etomoxir sodium salt) is an irreversible inhibitor of carnitine palmitoyltransferase-1 (CPT-1) on the outer face of the inner mitochondrial membrane. Etomoxir enhances palmitate-induced cell apoptosis.

Necrosulfonamide

Necrosulfonamide is a very specific and potent necrosis inhibitor and blocks mixed lineage kinase domain-like protein (MLKL).

CCT245737 (SRA737)

CCT245737 (SRA737) is an orally active CHK1 inhibitor with The IC50 of 1.4 nM. It exhibits >1,000-fold selectivity against CHK2 and CDK1.

Liraglutide

Liraglutide is a long-acting glucagon-like peptide-1(GLP-1) receptor agonist.

Tomivosertib (eFT508)

Tomivosertib (eFT-508) is a potent and selective MNK1/2 inhibitor with IC50s of 2.4 nM and 1 nM, respectively. It potentially results in decreased tumour cell proliferation and tumour growth. Tomivosertib (eFT-508) inhibits eIF4E phosphorylation and dramatically downregulates PD-L1 protein abundance.

Eganelisib (IPI-549)

Eganelisib (IPI-549) is a potent inhibitor of PI3K-γ with >100-fold selectivity over other lipid and protein kinases. The biochemical IC50 for PI3K-γ is 16 nM.

TAK-243 (MLN7243)

TAK-243 (MLN7243) is a potent, mechanism-based small-molecule inhibitor of the ubiquitin activating enzyme (UAE) with an IC50 of 1 ± 0.2 nM in the UBCH10 E2 thioester assay. It has minimal inhibitory activity in a panel of kinase and receptor assays, as well as on human carbonic anhydrase type I and type II. TAK-243 (MLN7243) induces ER stress, abrogates NF-κB pathway activation and promotes apoptosis.

PT2399

PT2399 is a potent and orally available antagonist of HIF-2 that selectively disrupts the heterodimerization of HIF-2α with HIF-1β.

WNK463

WNK463 is a pan-WNK-kinase inhibitor. It potently inhibits the in vitro kinase activity of all four WNK family members (WNK1, WNK2, WNK3, and WNK4) with IC50 of 5nM, 1nM, 6nM, and 9nM.

Tucatinib (Irbinitinib, ONT-380, Arry-380)

Tucatinib (Irbinitinib, ONT-380, ARRY-380) is an oral, potent, selective, reversible and ATP-competitive small-molecule inhibitor of ErbB-2 (also called HER2) with IC50s of 8 nM and 7 nM for ErbB-2 and p95 HER2, respectively in cell-based assays, showing ~500-fold selective for HER2 vs EGFR. It has potential antineoplastic activity.

S63845

S63845 is a new, selective MCL-1 inhibitor with the Kd value of 0.19 nM and has no discernible binding to the other Bcl-2 members, Bcl-2 or BCL-XL.

Eltanexor (KPT-8602)

Eltanexor (KPT-8602, ONO-7706, ATG-016) is a second-generation, orally bioavailable XPO1 (also known as CRM1) inhibitor with IC50 values of 20–211 nM in 10 AML lines after 3 days exposure.

Mivebresib (ABBV-075)

Mivebresib (ABBV-075) is a novel BET family bromodomain inhibitor. It binds bromodomains of BRD2/4/T with similar affinities (Ki of 1-2.2 nM) and is highly selective for 18 bromodomain proteins tested (Kd > 1 μM; more than 600-fold selectivity vs. BRD4), but exhibits roughly 10-fold weaker potency towards BRD3 (Ki of 12.2 nM) and has moderate activity towards CREBBP (Kd = 87 μM; 54-fold selectivity vs. BRD4). Mivebresib(ABBV-075) efficiently triggers apoptosis in various tumour cells.

Erdafitinib (JNJ-42756493)

Erdafitinib is a potent and selective orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity. Erdafitinib also binds to RET (c-RET), CSF-1R, PDGFR-α/PDGFR-β, FLT4, Kit (c-Kit) and VEGFR-2 and induces cellular apoptosis.

PACAP 1-38

PACAP 1-38 (Pituitary Adenylate Cyclase Activating Polypeptide 38) is a highly potent PACAP receptor agonist (Kd = 100 pM). It stimulates adenylate cyclase and phagocytosis.

FSL-1

FSL-1, a bacterial-derived toll-like receptor 2/6 (TLR2/6) agonist, enhances resistance to experimental HSV-2 infection.

RAD51 Inhibitor B02

B02 is a small-molecule inhibitor of human RAD51 with an IC50 of 27.4 μM, but does not inhibit its E. coli homologue RecA (IC50 > 250 μM).

CBL0137 Hydrochloride

CBL0137 (CBLC137, Curaxin 137) HCl activates p53 and inhibits NF-κB with EC50s of 0.37 μM and 0.47 μM in the cell-based p53 and NF-kB reporter assays, respectively. It also inhibits histone chaperone FACT (facilitates chromatin transcription complex).

AUNP-12

AUNP-12 (Aur-012, Aurigene-012, Aurigene NP-12), a new immune checkpoint modulator, is an inhibitor of the PD-1 pathway.

Avapritinib (BLU-285)

Avapritinib is a small molecule kinase inhibitor that potently inhibits PDGFR D842V mutant activity in vitro (IC50 = 0.5 nM) and PDGFR D842V autophosphorylation in the cellular setting (IC50 = 30 nM); also a potent inhibitor of the analogous Kit (c-Kit) mutation, D816V in Kit (c-Kit) Exon 17 (IC50 = 0.5 nM).

Verubecestat (MK-8931)

Verubecestat (MK-8931) is a potent and selective beta-secretase (also known as Beta-site APP-cleaving enzyme 1) inhibitor.

Nedisertib (M3814)

Nedisertib (M3814, Peposertib, MSC2490484A) is an orally bioavailable, highly potent and selective inhibitor of DNA activated protein kinase (DNA-PK) with IC50 of < 3 nM.

VX-984

VX-984 (M9831) is an orally active, potent, selective, and ATP-competitive inhibitor of DNA-PK. VX-984 effectively suppresses non-homologous end joining (NHEJ) and increases DNA double-strand breaks (DSBs). It enhances the cytotoxic effects of ionizing radiation (IR) in various cancer cell lines, including non-small cell lung cancer (NSCLC) cell lines, in vitro. Additionally, VX-984 reduces DNA-PKcs autophosphorylation.

Vorasidenib (AG-881)

Vorasidenib (AG-881) is an orally available inhibitor of mutated forms of both isocitrate dehydrogenase 1 and 2 (IDH1 and IDH2).

6-Diazo-5-oxo-L-norleucine (Diazooxonorleucine)

6-Diazo-5-oxo-L-norleucine (Diazooxonorleucine, L-6-Diazo-5-oxonorleucine, DON), an antibiotic isolated from Streptomyces, is a glutaminase antagonist with IC50 of ~1 mM for cKGA (kidney-type glutaminase). 6-Diazo-5-oxo-L-norleucine exhibits analgesic, antibacterial, antiviral and anticancer properties.

Necrostatin 2 racemate (Nec-1s)

Necrostatin 2 racemate (Nec-1s, 7-Cl-O-Nec1, Necrostatin-1 stable, Necrostatin 1S) is a stable variant of Necrostatin-1. It is a more specific RIPK1 inhibitor lacking the IDO-targeting effect, with >1000-fold more selective for RIPK1 than for any other kinase out of 485 human kinases.

bpV (HOpic)

bpV (HOpic) (Bisperoxovanadium (HOpic)) is a potent inhibitor of PTEN with an IC50 of 14 nM. The IC50s for PTP-β and PTP-1B are about 350- and 1800-fold higher than the IC50 for PTEN, respectively.

CA3 (CIL56)

CA3 (CIL56) has potent inhibitory effects on YAP1/Tead transcriptional activity and primarily targets YAP1 high and therapy-resistant esophageal adenocarcinoma cells endowed with CSC properties. CA3(CIL56) induces Ferroptosis and iron-dependent reactive oxygen species (ROS).

GSK3326595 (Pemrametostat, EPZ015938)

Pemrametostat (GSK3326595, EPZ015938) is an orally active, potent and selective inhibitor of protein arginine methyltransferase 5 (PRMT5) and potently inhibits tumour growth in vitro and in vivo in animal models.

JPH203 (Nanvuranlat)

Nanvuranlat (JPH203, KYT-0353, JPH-203SBECD), a selective L-type amino acid transporter 1 inhibitor, shows a dramatic inhibition of leucine uptake (IC50=0.06 µM) and cell growth (IC50=4.1 µM) in human colon cancer cells (HT-29), human oral cancer cells (YD-38) and leukemic cells.

GDC-0077 (Inavolisib)

Inavolisib (GDC-0077, RG6114, RO-7113755) is a potent selective inhibitor of PI3K alpha (PI3Kα) with an IC50 of 0.038 nM. GDC-0077 is >300-fold more selective for PI3K alpha over the other class I PI3K isoforms (beta, delta, and gamma) and >2000-fold more selective over PIK family members. GDC-0077 binds to the ATP binding site of PI3K and inhibits the phosphorylation of PIP2 to PIP3.

ONC212

ONC212, a fluorinated-ONC201 analogue, is a selective agonist of GPR132. ONC212 is broadly efficacious across most solid tumours and haematological malignancies in the low nanomolar range and has robust anti-leukaemic activity.

GO-203 TFA

GO-203 is a D-amino acid cell-penetrating peptide inhibitor of MUC1-C dimerization and thereby its oncogenic function.

AZD1390

AZD1390 is a first-in-class orally available and CNS penetrant ATM inhibitor with an IC50 of 0.78 nM in cells and >10,000-fold selectivity over closely related members of the PIKK family of enzymes and excellent selectivity across a broad panel of kinases.

MPP dihydrochloride

Methyl-piperidino-pyrazole (MPP) dihydrochloride is a highly selective antagonist for estrogen receptor alpha (ERα), with an affinity 200 times greater than for estrogen receptor beta (ERβ). It inhibits 17β-estradiol binding to ERα by inducing conformational changes that alter the receptor’s binding site and also increases the energy required for genistein's interaction with ERα.

AZD4573

AZD4573 is a potent inhibitor of CDK9 (IC50 of <0.004 μM) with fast-off binding kinetics (t_1/2 = 16 min) and high selectivity versus other kinases, including other CDK family kinases.

Samuraciclib (ICEC0942) hydrochloride

Samuraciclib (ICEC0942) hydrochloride is a new, orally bioavailable CDK7 inhibitor with an IC50 of 40nM. The IC50 values for CDK1, CDK2, CDK5 and CDK9 were 45-, 15-, 230- and 30-fold higher. ICEC0942 (CT7001) promotes cell cycle arrest and apoptosis.

Lazertinib (YH25448)

Lazertinib (YH25448,GNS-1480) is a potent, highly mutant-selective and irreversible EGFR-TKI with IC50 values of 1.7 nM, 2 nM, 5 nM, 20.6 nM and 76 nM for Del19/T790M, L858R/T790M, Del19, L85R and Wild type EGFR respectively, showing much higher IC50 values aganist ErbB2 and ErbB4.

Enitociclib (BAY 1251152)

Enitociclib (BAY 1251152) is a potent PTEFb/CDK9 inhibitor with an IC50 value of 3 nM for CDK9 and an at least 50-fold selectivity against other CDKs in enzymatic assays. BAY1251152 binds to and blocks the phosphorylation and kinase activity of CDK9, thereby preventing PTEFb-mediated activation of RNA Pol II and leading to the inhibition of gene transcription of various anti-apoptotic proteins.

IACS-010759 (IACS-10759)

IACS-010759 (IACS-10759) is a potent and selective oxidative phosphorylation inhibitor (IC50 < 10 nM) that blocks cellular respiration through inhibition of complex I.

A-485

A-485 is a potent, selective and drug-like p300/CBP catalytic inhibitor with an IC50 of 0.06 μM for p300 HAT. It is selective over BET bromodomain proteins and >150 non-epigenetic targets.

INCB054329

INCB054329 is a structurally distinct bromodomain and extraterminal domain (BET) inhibitor with IC50 values of 44 nM, 5 nM, 9 nM, 1 nM, 28 nM, 3 nM, 119 nM and 63 nM for BRD2-BD1, BRD2-BD2, BRD3-BD1, BRD3-BD2, BRD4-BD1, BRD4-BD2, BRDT-BD1 and BRDT-BD2, respectively.

Iberdomide (CC-220)

Iberdomide (CC-220) is a novel oral immunomodulatory compound that targets cereblon, part of the CRL4CRBN E3 ubiquitin ligase complex, with an IC50 of 60 nM in a competitive TR-FRET assay. Iberdomide (CC-220) induces apoptosis with antitumor and immunostimulatory activities.

dBET6

dBET6 is a highly cell-permeable PROTAC degrader of BET bromodomains with an IC50 of 14 nM for BRD4 binding. dBET6 also induces c-MYC downregulation and apoptosis.

DT-061 (SMAP)

DT-061 (SMAP) is a bioavailable PP2A activator. It decreases cell viability in HCC827 and HCC3255 cell lines, with IC50 values of 14.3 μM and 12.4 μM respectively.

ML385

ML385 is a novel and specific NRF2 inhibitor with an IC50 of 1.9 μM. It inhibits the downstream target gene expression of NRF2. NRF2 regulates the activity of several Ferroptosis and lipid peroxidation-related proteins.

diABZI STING agonist-1 (tautomerism)

diABZI STING agonist (diABZI STING agonist-1, Compound 3, Tautomerism) is a potent non-nucleotide STING agonist and has tremendous potential to improve treatment of cancer in humans.Solutions are unstable and should be fresh-prepared.

V-9302

V-9302 is a competitive small molecule antagonist of transmembrane glutamine flux, that selectively and potently targets the amino acid transporter ASCT2 (SLC1A5) with an IC50 value of 9.6 μM for inhibition of glutamine uptake in HEK-293 cells. V-9302 blocks Sodium-neutral AA transporter 2 (SNAT2, SLC38A2) and the large neutral AA transporter 1 (LAT1, SLC7A5) as observed in 143B osteosarcoma cells, HCC1806 breast cancer cells and Xenopus laevis oocytes. Dilution of PBS may cause a clear aqueous solution to turn into a uniform suspension.

Subasumstat (TAK-981)

Subasumstat (TAK-981) is a novel, selective inhibitor of the SUMOylation enzymatic cascade with potential immune-activating and antineoplastic activities.

AMG 510 (Sotorasib)

Sotorasib (AMG510) is a potent KRAS G12C covalent inhibitor with potential antineoplastic activity.This AMG510 is a chiral compound.

SEL120 (SEL120-34A) hydrochloride

SEL120 (SEL120-34, SEL120-34A) is a novel inhibitor of Cyclin-dependent kinase 8 (CDK8) with IC50 values of 4.4 nM and 10.4 nM for CDK8/Cyclin C and CDK19/CyclinC respectively.

AZD7648

AZD7648 is a potent inhibitor of DNA-PK with an IC50 of 0.6 nM in biochemical assay and more than 100-fold selective against 396 other kinases.

VX-445 (Elexacaftor)

Elexacaftor (VX-445) is a next-generation cystic fibrosis transmembrane conductance regulator (CFTR) corrector.This is a compound which is not chiral purity.

Imidazole Ketone Erastin (IKE)

Imidazole Ketone Erastin (IKE) is a potent, selective, and metabolically stable system xc– inhibitor and inducer of Ferroptosis.

BMS-986165 (Deucravacitinib)

Deucravacitinib (BMS-986165) is a highly potent and selective allosteric inhibitor of Tyk2 with a Ki value of 0.02 nM for binding to the Tyk2 pseudokinase domain. It is highly selective against a panel of 265 kinases and pseudokinases.

LLY-283

LLY-283 is a novel and selective inhibitor of protein arginine methyltransferase 5 (PRMT5). LLY-283 inhibits PRMT5 enzymatic activity in vitro and in cells with IC50 of 22 nM and 25 nM, respectively. LLY-283 shows antitumor activity.

Adagrasib (MRTX849)

Adagrasib (MRTX849) is a potent, selective, and covalent KRASG12C inhibitor that exhibits favourable drug-like properties, selectively modifies mutant cysteine 12 in GDP-bound KRASG12C and inhibits KRAS-dependent signalling.

PT2977 (Belzutifan)

Belzutifan (PT2977), an orally active and selective HIF-2α inhibitor, increases potency and improves pharmacokinetic profile, providing a potential treatment for clear cell renal cell carcinoma (ccRCC).

Firsocostat (ND-630, GS-0976)

Firsocostat (GS-0976, ND-630) is a reversible inhibitor of acetyl CoA carboxylase (ACC) with IC50s of 2.1 nM, 6.1 nM for hACC1 and hACC2, respectively.

AS2863619

AS2863619 is a small-molecule cyclin-dependent kinase CDK8/19 inhibitor with IC50 of 0.6099 nM and 4.277 nM, respectively. AS2863619 is a potent Foxp3 inducer in T_conv cells.

MYCi975

MYCi975 (NUCC-0200975) is a potent, selective and orally active inhibitor of MYC that disrupts MYC/MAX interaction, promotes MYC T58 phosphorylation and MYC degradation, and impairs MYC driven gene expression. MYCi975 exhibits potent anti-tumour activities.

TBK1/IKKε-IN-5

TBK1/IKK -IN-5 (compound 1) is a dual inhibitor of TANK-binding kinase 1 (TBK1) and I B kinase- (IKK /IKK-i) with IC50 of 1.0 nM and 5.6 nM for TBK1 and IKK , respectively. TBK1/IKK inhibition enhances response to PD-1 blockade, which effectively predicts tumour response in vivo.

Valemetostat (DS-3201)

Valemetostat (DS-3201, DS-3201b) is a selective EZH1/2 dual inhibitor.

MCC950

MCC950 (CP-456773, CRID3) is a potent and selective inhibitor of NLRP3 (NOD-like receptor (NLR) family, pyrin domain-containing protein 3) with IC50 of 7.5 nM and 8.1 nM in BMDMs and HMDMs, respectively.

(Z)-4-Hydroxytamoxifen

(Z)-4-Hydroxytamoxifen ((Z)-4-OHT, trans-4-Hydroxytamoxifen, 4-Monohydroxytamoxifen) is a selective modulator of estrogen receptor (SERM) with IC50 of 3.3 nM for the [³H]oestradiol binding to oestrogen receptor.

BI-2852

BI-2852 is a potent inhibitor of KRAS that binds with nanomolar affinity to a pocket between switch I and II on RAS. BI-2852 blocks all GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signalling and an antiproliferative effect in the low micromolar range in KRAS mutant cells.

CD38 inhibitor 1 (compound 78c)

CD38 inhibitor 1 (compound 78c, CD38-IN-78c, MDK-7553) is a potent inhibitor of CD38 with IC50 of 7.3 nM and 1.9 nM for human CD38 and mouse CD38, respectively.

Actinomycin D (Dactinomycin)

Actinomycin D (Dactinomycin, Act D, RASP-101) is a significant polypeptide antibiotic isolated from soil bacteria of the genus Streptomyces. Actinomycin D (Dactinomycin) inhibits DNA repair and rests the cell cycle at G1 phase with IC50 of 0.42 μM and 0.4 nM, respectively. Actinomycin D is an RNA and protein synthesis inhibitor that can suppress bacterial protein synthesis. Actinomycin D is an autophagy activator, induces p53-independent cell death and prolongs survival in high-risk chronic lymphocytic leukemia.This product is a hazardous chemical (acute toxicity/flammable/skin corrosive). Please use it while wearing a protective face mask, gloves, and clothing.

PRI-724 (Foscenvivint)

Foscenvivint (PRI-724) is a potent and specific inhibitor that disrupts the interaction of β-catenin and CBP.

Molnupiravir (EIDD-2801)

Molnupiravir (EIDD-2801, MK-4482) is an orally bioavailable prodrug of the ribonucleoside analog β-d-N⁴-hydroxycytidine (NHC; EIDD-1931) with broad-spectrum antiviral activity against SARS-CoV-2, MERS-CoV, SARS-CoV, and the causative agent of COVID-19.

MitoQ (Mitoquinone) Mesylate

MitoQ (Mitoquinone) Mesylate is a TPP-based, mitochondria-targeted antioxidant that blocks H₂O₂-induced intracellular ROS responses and protects against oxidative damage. This product is a waxy solid.

Zotatifin (eFT226)

Zotatifin (eFT226) is a highly effective and sequence-selective inhibitor of the RNA helicase eIF4A. It promotes eIF4A binding to specific mRNA sequences with recognition motifs in the 5'-UTRs, with an IC50 of 2 nM, and disrupts the assembly of the eIF4F initiation complex. By enhancing the interaction between eIF4A and polypurine RNA sequence or structural motifs, zotatifin converts eIF4A into a sequence-specific translation repressor, thereby regulating the translation of certain target genes. It also exhibits anti-tumour activity.

BAY 2416964

BAY 2416964 (compound 192) is a potent and orally active antagonist of aryl hydrocarbon receptor (AhR) with IC50 of 341 nM. BAY 2416964 has the potential in the treatment of solid tumours.

SNDX-5613 (Revumenib)

Revumenib (SNDX-5613) is a potent and selective inhibitor of menin-MLL binding with a Ki of 0.15 nM. SNDX-5613 shows anti-proliferative activity against multiple cell lines harbouring MLLr translocations (MV4;11, RS4;11, MOLM-13, KOPN-8) with IC50 values ranging from 10-20 nM.

Wedelolactone

Wedelolactone, a medicinal plant-derived natural compound, is an inhibitor of IKK that is critical for activation of NF-κB by mediating phosphorylation and degradation of IκBα. Wedelolactone is also an inhibitor of caspase-11.

CC-90001

CC-90001 is an orally administered inhibitor of c-Jun N-terminal kinase (JNK) with bias for JNK1 over JNK2. It exhibits antifibrotic efficacy and can be used for the research of idiopathic pulmonary fibrosis.

Elacestrant (RAD1901) Dihydrochloride

Elacestrant (RAD1901) Dihydrochloride is an orally available selective estrogen receptor degrader (SERD) with IC50 of 48 nM and 870 nM for ERα and ERβ, respectively.

PF-06821497

PF-06821497 is a selective and orally active inhibitor of Zeste Homolog 2 (EZH2) with a Ki value <0.1 nM against mutant Y641N EZH2. It exhibits robust tumour growth inhibition.

UNC2025

UNC2025 is a potent and orally active dual inhibitor of FLT3 and MER with IC50 of 0.35 nM and 0.46 nM, respectively. UNC2025 also inhibits AXL, TRKA, TRKC, QIK, TYRO3, SLK, NuaK1, Kit (c-Kit) and Met (c-Met) with IC50 of 1.65 nM, 1.67 nM, 4.38 nM, 5.75 nM, 5.83 nM, 6.14 nM, 7.97 nM, 8.18 nM and 364 nM, respectively.

Inobrodib (CCS-1477)

Inobrodib (CCS1477; CBP-IN-1; CBP/p300-IN-4) is a potent and selective inhibitor of p300/CBP bromodomain. CCS1477 works by inhibiting the expression and function of the Androgen Receptor (AR), as well as inhibiting c-Myc.

Semaglutide

Semaglutide is an oral agonist of glucagon-like peptide-1 receptor (GLP1R), used for treating type 2 diabetes and obesity by enhancing insulin secretion, reducing glucagon levels, and promoting weight loss. It is available in subcutaneous and oral formulations.

Ezatiostat

Ezatiostat, a tripeptide analog of glutathione, is a peptidomimetic inhibitor of Glutathione S-transferase P1-1 (GSTP1-1). Ezatiostat activates c-Jun NH2 terminal kinase (JNK1) and ERK1/ERK2 and induces Apoptosis.

OT-82

OT-82 is a novel nicotinamide phosphoribosyltransferase (NAMPT) inhibitor with average IC50s of 13.03 nM in non-HP cancer cells and 2.89 nM in HP cancer cells, respectively.

Denifanstat (TVB-2640)

Denifanstat (TVB-2640) is an orally bioavailable, pharmacological fatty acid synthase (FAS/FASN) inhibitor with therapeutic potential in patients with NAFLD and nonalcoholic steatohepatitis.

Rimiducid (AP1903)

Rimiducid (AP1903) is a chemical protein dimerizer and binds tightly to the target FKBP fusion protein while binding minimally to the abundant natural FKBP. Rimiducid elicits potent and dose-dependent Apoptosis of cells in culture expressing dimerizer-dependent Fas constructs, with an EC50 of ≈0.1 nM.

Bomedemstat (IMG-7289)

Bomedemstat (IMG-7289) is an orally active and irreversible inhibitor of LSD1 (lysine-specific demethylase 1). Bomedemstat exhibits the ability to enhance methylation levels of H3K4 and H3K9, subsequently leading to modifications in gene expression. Bomedemstat demonstrates anti-cancer properties by restraining cancer cell proliferation and prompting apoptosis.

ME-344

ME-344 is a synthetic metabolite of NV-128, a potent inhibitor of mitochondrial oxidative phosphorylation (OXPHOS) complex I, disrupting ATP generation and oxygen consumption. It also inhibits mTOR by downregulating the AKT/mTOR pathway, exhibiting anticancer activity by inhibiting cell growth and viability in leukaemia cell lines with IC50 values of 70–260 nM.

4-HNE (4-Hydroxynonenal)

4-HNE (4-Hydroxynonenal) is one of the major end products of lipid peroxidation and has been widely accepted as an inducer of oxidative stress.

IXA4

IXA4, a highly selective, non-toxic IRE1/XBP1s activator, activates IRE1/XBP1s signaling without globally activating the unfolded protein response (UPR) or other stress-responsive signaling pathways, and reduces secretion of amyloid precursor protein (APP) through IRE1 activation, preventing APP-associated mitochondrial dysfunction.

Elamipretide (SS-31, MTP-131)

Elamipretide (MTP-131, SS-31) is a cytochrome c peroxidase inhibitor. Elamipretide improves mitochondrial dysfunction, synaptic and memory impairment induced by lipopolysaccharide in mice.

dTAG-13

dTAG-13(FKBP12 PROTAC dTAG-13) is an ortho-substituted, heterobifunctional selective degrader of FKBP12^F36V that effectively engage FKBP12F36V and CRBN leading to rapid and selective CRBN-mediated degradation of FKBP12F36V.It can useful for target validation in the context of drug discovery.

Danuglipron (PF-06882961)

Danuglipron (PF-06882961), a non-peptide agonist, activates the canonical G protein signalling activity only in the Glucagon-like peptide-1 (GLP-1) receptor with Trp33^ECD.

Orforglipron (LY3502970)

Orforglipron (LY3502970) is a non-peptidal agonist of glucagon-like peptide 1 (GLP-1) receptor. It can be used efficiently in glycaemic control and weight reduction in type 2 diabetes mellitus (T2DM), obesity or both.

Vepdegestrant (ARV-471)

Vepdegestrant (ARV471) is an orally bioavailable estrogen receptor-targeting (ER-targeting) PROTAC for the treatment of patients with locally advanced or metastatic ER+/HER2- breast cancer.

STM2457

STM2457 is a highly potent and selective first-in-class catalytic inhibitor of RNA Methyltransferase METTL3 with an IC50 of 16.9 nM. STM2457 is highly specific for METTL3 and showed no inhibition of other RNA methyltransferases.

AG-270

AG-270 is a potent and non-competitive methionine adenosyltransferase 2A (MAT2A) inhibitor which lessens the intracellular SAM levels and MTAP-null–selective antiproliferative activity.

AZD5305 (Saruparib)

Saruparib (AZD5305) is a highly selective and potent inhibitor of PARP1 with an IC50 of 3 nM in wild-type A549 lung cancer cells. AZD5305 shows no or minimal growth inhibitory effects in other cells (IC50s >10μM).

Tagtociclib (PF-07104091)

Tagtociclib (PF-07104091) inhibits CDK2, which may result in cell cycle arrest, induction of apoptosis, and inhibition of tumour cell proliferation.

ART558

ART558 is a potent, selective, low molecular weight, allosteric inhibitor of DNA Polθ with an IC50 of 7.9 nM.

Danicamtiv (MYK-491)

Danicamtiv (MYK-491, SAR 440181) is a novel cardiac myosin activator that enhances cardiomyocyte contraction.

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