Kinases & Cell Signaling

KPT-6566

CAS 881487-77-0

KPT-6566 is a covalent PIN1 inhibitor for cancer signaling research. Published studies connect PIN1 inhibition with oxidative stress, DNA damage, cancer-cell death and reduced lung colonization in mice.

CHIR-99021 (CT99021)

CAS 252917-06-9

CHIR-99021 (CT99021) is a GSK-3 inhibitor used in signaling, cell-state and metabolic research.

Y-27632 dihydrochloride

CAS 129830-38-2

Y-27632 dihydrochloride is a ROCK inhibitor for cell-survival and cytoskeletal research, including dissociated human pluripotent stem-cell cultures.

JTE-013

CAS 383150-41-2

JTE-013 is an S1PR2 antagonist used in sphingosine-1-phosphate signaling, mitochondrial dynamics and fibrosis research.

BAY-3827

CAS 2377576-35-5

BAY-3827 is an AMPK inhibitor with additional RSK-family activity, used to study metabolic signaling and androgen-dependent prostate cancer.

ζ-Stat (ZETA-STAT)

CAS 3316-02-7

ζ-Stat (ZETA-STAT) is a research inhibitor investigated in atypical PKC signaling and invasive behavior of clear-cell ovarian cancer cells.

PF-543

CAS 1415562-82-1

PF-543 is a potent, sphingosine-competitive SPHK1 inhibitor for investigating S1P production and sphingolipid signaling.

ABC 1183

CAS 1042735-18-1

ABC 1183 (ABC1183) is a dual GSK-3/CDK9 inhibitor for cancer-cell proliferation and inflammatory signaling research.

Praliciguat

CAS 1628730-49-3

Praliciguat is an sGC stimulator for nitric-oxide/cGMP signaling, renal inflammation and fibrosis research.

9-ING-41

CAS 1034895-42-5

9-ING-41 (Elraglusib) is a cancer-research compound originally developed as a GSK-3β inhibitor. Published work documents model-dependent growth inhibition and additional mechanisms.

JP-153

CAS 1802937-26-3

JP-153 is a focal-adhesion-signaling modulator for VEGF-dependent retinal endothelial-cell and angiogenesis research.

MK-8722

CAS 1394371-71-1

MK-8722 is a direct allosteric activator of mammalian AMPK complexes for metabolic signaling and glucose-homeostasis research.

BL-AD008

BL-AD008 is an AMPK/ZIPK-directed activator investigated in cervical-cancer apoptosis research.

Sulfopin

CAS 2451481-08-4

Sulfopin is a covalent PIN1 inhibitor used to study prolyl-isomerase signaling and MYC-driven cancer biology.

Adavivint

CAS 1467093-03-3

Adavivint is a potent and selective inhibitor of canonical Wnt signaling, with an EC50 of 19.5 nM via a high-throughput TCF/LEF-reporter assay in SW480 colon cancer cells.

WZ4002

CAS 1213269-23-8

WZ4002 is a mutant selective EGFR inhibitor with IC50s of 2, 8, 3 and 2 nM for EGFRL858R, EGFRL858R/T790M, EGFRE746_A750 and EGFRE746_A750/T790M, respectively.

GW788388

CAS 452342-67-5

GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM, and also inhibits TGF-β type II receptor and activin type II receptor activities, without inhibiting BMP type II receptor.

AZD1152

CAS 722543-31-9

AZD1152 is a pro-drug of Barasertib-hQPA, which is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay.

MTX211

CAS 1952236-05-3

MTX-211 is a dual inhibitor of EGFR and PI3K, used for the treatment of cancer and other diseases.

GNF-2

CAS 778270-11-4

GNF-2 is a highly selective non-ATP competitive inhibitor of oncogenic Bcr-Abl activity (IC50 = 0.14 μM).IC50 value: 0.14 uM [1]Target: Bcr-Ablin vitro: Ba/F3 cells harboring native or T315I mutated Bcr-Abl constructs were treated with GNF-2 and AKIs. We…

Canertinib dihydrochloride

CAS 289499-45-2

Canertinib dihydrochloride (CI-1033;PD-183805) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC50s of 7.4 and 9 nM.

CGK733

CAS 905973-89-9

CGK733 is a potent ATM/ATR inhibitor, used for the research of cancer.

PF-670462

CAS 950912-80-8

PF-670462 is a potent and selective inhibitor of casein kinase (CK1ε and CK1δ), with IC50s of 7.7 nM and 14 nM, respectively.

BMS-833923 (XL-139)

CAS 1059734-66-5

BMS-833923 (XL-139) is an orally bioavailable small-molecule inhibitor of Smoothened with potential antineoplastic activity; inhibits BODIPY cyclopamine binding to SMO in a dose-dependent manner with an IC50 of 21 nM.BMS-833923 inhibits the sonic hedgehog…

Merestinib(LY2801653 dihydrochloride)

CAS 1206801-37-7

Merestinib dihydrochloride (LY2801653 dihydrochloride) is a type-II ATP competitive, slow-off inhibitor of MET tyrosine kinase with a dissociation constant (Ki) of 2 nM.

FLLL32

CAS 1226895-15-3

FLLL32 is a STAT3 inhibitor derived from the natural product curcumin. FLLL32 retains the cellular response to cytokines with anti-tumor activity[1].

LY2835219 free base (Abemaciclib)

CAS 1231929-97-7

Abemaciclib (LY2835219) is a selective CDK4/6 inhibitor with IC50 values of 2 nM and 10 nM for CDK4 and CDK6, respectively.

PKG drug G1

CAS 374703-78-3

PKG drug G1 targets C42 of PKG Iα. PKG drug G1 can couple to vasodilation and blood pressure lowering by a C42 PKG Iα-independent mechanism.

AZD2932

CAS 883986-34-3

AZD2932 is a potent and multi-targeted kinase inhibitor VEGFR2, PDGFβ, Flt-3 and c-Kit with IC50s of 8, 4, 7 and 9 nM in cell assay, respectively.

PD153035 HCl (SU-5271, AG1517)

CAS 183322-45-4

PD153035 (ZM 252868;AG 1517;Tyrphostin AG 1517;SU 5271) is a potent EGFR inhibitor with Ki and IC50 of 6 and 25 pM, respectively.

CID-2011756

CAS 638156-11-3

CID 2011756 is an ATP competitive PKD inhibitor, with an IC50 of 3.2 µM for PKD1 in cell free assay, and also shows cellular pan-PKD inhibitory activity against PKD2 and PKD3 (IC50, 0.6 and 0.7 µM, respectively). CID 2011756 also has antitumor activity.

Tenovin-3

CAS 1011301-27-1

Tenovin-3 is able to increase p53 levels, determined in MCF-7 cells treated for 6 hr at 10 μM.Target: p53in vitro: Tenovins inhibit the activities of human SirT1 and SirT2, two members of the NAD+-dependent class III histone deacetylases that also belong to…

NVP-AEW541

CAS 475489-16-8

NVP-AEW541 is a potent inhibitor of IGF-1R with IC50 of 0.15 μM, also inhibits InsR, with IC50 of 0.14 μM.

Rociletinib (CO-1686)

CAS 1374640-70-6

Rociletinib (CO-1686) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.

GNE-7915

CAS 1351761-44-8

GNE-7915 is a potent, selective and brain-penetrant inhibitor of LRRK2 with an IC50 of 9 nM.

AMG-510(Sotorasib)

CAS 2296729-00-3

AMG-510 is a specific covalent inhibitor of K-RAS(G12C) with potential antineoplastic activity. Upon oral administration, KRAS mutant-targeting AMG-510 selectively targets the KRAS p.G12C mutant, at either the DNA, RNA or protein level, and prevents, thro

CH5424802(Alectinib)

CAS 1256580-46-7

The dissociation constant (KD) value of CH5424802 For ALK in an ATP-competitive manner is 2.4 nM. CH5424802 has substantial inhibitory potency against both native ALK and L1196M with Ki of 0.83 nM and 1.56 nM, respectively. CH5424802 prevents…

ISRIB

CAS 1597403-47-8

ISRIB (trans-isomer) is a potent inhibitor of PERK with an IC50 of 5 nM.

R1530

CAS 882531-87-5

R1530 is the multikinase inhibitor with potential antiangiogenesis and antineoplastic activities.R1530 is also a mitosis-angiogenesis inhibitor (MAI) that inhibits multiple receptor tyrosine kinases involved in angiogenesis, such as vascular endothelial…

AZ5104

CAS 1421373-98-9

AZ-5104 is an active, demethylated metabolite of AZD 9291. AZ-5104 is an EGFR inhibitor with IC50s of 1, 6, 1, 25 and 7 nM for EGFRL858R/T790M, EGFRL858R, EGFRL861Q, EGFR and ErbB4, respectively.

AT7519 HCL

CAS 902135-91-5

AT7519 Hydrochloride is a potent inhibitor of CDKs, with IC50s of 210, 47, 100, 13, 170, and <10 nM for CDK1, CDK2, CDK4 to CDK6, and CDK9, respectively.

YC-1(Lificiguat)

CAS 170632-47-0

Lificiguat binds to the β subunit of soluble guanylyl cyclase(sGC) with Kd of 0.6-1.1 μM in the presence of CO.

SB 239063

CAS 193551-21-2

SB 239063 is a potent and selective p38 MAPK inhibitor (IC50 = 44 nM for p38α). SB 239063 displays > 220-fold selectivity over ERK, JNK1 and other kinases; ~ 3-fold more selective than SB 203580. IC50 value: 44 nM ( p38α)Target: p38 MAPKSB 239063 reduces…

FK-506 (Tacrolimus)

CAS 104987-11-3

Tacrolimus is a macrocyclic lactone with potent immunosuppressive properties. Tacrolimus binds to FK506 binding protein (FKBP) to form a complex and inhibits calcineurin phosphatase.

SMI 4a

CAS 438190-29-5

(Z)-SMI-4a is a selective ATP-competitive Pim-1 kinase inhibitor with an IC50 of 21 nM for Pim-1 compared to an IC50 of 100 nM for Pim-2 and with little or no activity against a panel of 50 other kinases tested.

GSK2636771

CAS 1372540-25-4

GSK2636771 is a potent, selective and oral inhibitor of PI3Kβ with a Ki of 0.89 nM and an IC50 of 5.2 nM, showing 900-fold selectivity over p110α and p110γ, and 10-fold selectivity over p110δ isoforms.

ZM306416

CAS 690206-97-4

ZM-306416 (CB 676475) is a potent inhibitor of VEGFR with IC50s of 0.1 and 2 μM for KDR and Flt, respectively. ZM-306416 is also a EGFR inhibitor with an IC50 of <10 nM.

TAK-632

CAS 1228591-30-7

TAK-632 is a potent pan-RAF inhibitor with IC50 of 1.4, 2.4 and 8.3 nM for CRAF, BRAFV600E, BRAFWT, respectively.