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Chk Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
S1532 AZD7762 AZD7762 is a potent and selective inhibitor of Chk1 with IC50 of 5 nM in a cell-free assay. It is equally potent against Chk2 and less potent against CAM, Yes, Fyn, Lyn, Hck and Lck. Phase 1.
EMBO Rep, 2025, 26(14):3574-3593
Mol Cell Proteomics, 2025, 24(3):100915
PLoS One, 2025, 20(6):e0324443
Verified customer review of AZD7762
S2626 Rabusertib (LY2603618) Rabusertib (LY2603618, IC-83) is a highly selective Chk1 inhibitor with potential anti-tumor activity in a cell-free assay. IC50=7 nM, showing approximately 100-fold more potent against Chk1 than against any of the other protein kinases evaluated. Rabusertib (LY2603618) induces cell cycle arrest, DNA damage response and autophagy in cancer cells. Rabusertib (LY2603618) induces bak-dependent apoptosis in AML cell lines.
Nat Commun, 2025, 16(1):5706
Nat Commun, 2025, 16(1):480
Nucleic Acids Res, 2025, 53(12)gkaf544
Verified customer review of Rabusertib (LY2603618)
S2735 MK-8776 (SCH 900776) MK-8776 (SCH 900776) is a selective Chk1 inhibitor with IC50 of 3 nM in a cell-free assay, showing 500-fold selectivity against Chk2. It is in Phase 2.
Mol Cell, 2025, 85(13):2474-2486.e6
Cell Rep Med, 2025, 6(8):102284
Cell Rep Med, 2025, S2666-3791(25)00231-9
Verified customer review of MK-8776 (SCH 900776)
S2683 CHIR-124 CHIR-124 is a novel and potent Chk1 inhibitor with IC50 of 0.3 nM in a cell-free assay. It shows 2,000-fold selectivity against Chk2, 500- to 5,000-fold less activity against CDK2/4 and Cdc2.
Cell Rep Med, 2025, S2666-3791(25)00102-8
Cell Rep, 2025, 44(8):116019
Nature, 2024, 635(8037):210-218
Verified customer review of CHIR-124
S7178 Prexasertib (LY2606368) Dihydrochloride Prexasertib HCl (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.
J Exp Clin Cancer Res, 2025, 44(1):163
J Exp Clin Cancer Res, 2025, 44(1):271
Science, 2024, 384(6700):eadk0775
Verified customer review of Prexasertib (LY2606368) Dihydrochloride
S2904 PF-477736 PF-477736 (PF-736, PF-00477736) is a selective, potent and ATP-competitive Chk1 inhibitor with Ki of 0.49 nM in a cell-free assay and also inhibits VEGFR2, Aurora-A, FGFR3, Flt3, Fms (CSF1R), Ret and Yes. It shows ~100-fold selectivity for Chk1 than Chk2.
Hematol Oncol, 2025, 43(5):e70131
Nat Commun, 2024, 15(1):8890
Cell Rep Med, 2024, 5(10):101778
Verified customer review of PF-477736
S6385 Prexasertib (LY2606368)

Prexasertib (LY2606368, ACR 368) is a selective ATP competitor inhibitor of Chk1 and Chk2 with IC50s of 1 nM and 8 nM in cell-free assays, respectively. Prexasertib also inhibits RSK1 with an IC50 of 9 nM in cell-free assay.
Cell Rep Med, 2025, S2666-3791(25)00151-X
Mol Oncol, 2025, 19(6):1633-1650
Biomol Ther (Seoul), 2025, 33(3):458-469
S8632 BML-277 (Chk2 Inhibitor II) BML-277 (Chk2 Inhibitor II) is an ATP-competitive inhibitor of Chk2 with IC50 of 15 nM, and it is 1000-fold more selective toward Chk2 serine/threonine kinase than for Chk1 and Cdk1/B kinases. This compound dose dependently protects human CD4(+) and CD8(+) T-cells from apoptosis due to ionizing radiation.
BMC Cancer, 2025, 25(1):1520
Sci Adv, 2025, 11(30):eadu9555
Int J Mol Sci, 2024, 25(17)9473
S8253 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.
bioRxiv, 2024, 2024.05.03.592420
Mol Oncol, 2023, 10.1002/1878-0261.13537
Biochem J, 2022, 479(19):2063-2086
S8526 GDC-0575 GDC-0575 is a potent and selective CHK1 inhibitor with an IC50 of 1.2 nM.
Front Cardiovasc Med, 2023, 10:1187490
J Exp Clin Cancer Res, 2022, 41(1):141
Biochem Biophys Res Commun, 2021, 584:7-14
E1991 BBI-355 BBI-355 is an oral, potent, and selective small molecule inhibitor of CHK1 with an IC50 of 0.3 nM. It demonstrates significant anti-tumor activity as a single agent and in combination with targeted therapies in multiple ecDNA+ oncogene amplified tumor models.
E1653 CCT241533 hydrochloride CCT241533 hydrochloride is an ATP competitive, potent, and selective inhibitor of CHK2 with an IC50 of 3 nM and a Ki of 1.16 nM and shows minimal cross-reactivity against a panel of kinases. CCT241533 inhibits CHK2 activity in human tumor cell lines when subjected to DNA damage.
S7740 SAR-020106 SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC50 of 13.3 nM.
E5832New BBI-2779 BBI-2779 is a potent, selective, and orally active inhibitor of CHK1 with an IC50 of 0.3 nM. It preferentially kills cancer cells containing extrachromosomal DNA (ecDNA) by inducing replication stress and cell death. In gastric cancer models with FGFR2 gene amplification on ecDNA, BBI-2779 suppresses tumor growth and prevents drug resistance.
E1667 LY2880070 LY2880070 is an orally active inhibitor of CHK1. This compound can be used as an anticancer agent and shows promise in preclinical models of pancreatic ductal adenocarcinoma (PDAC) when used in combination with DNA-damaging agents.
S8148 PD0166285 PD0166285 is a potent Wee1 and Chk1 inhibitor with activity at nanomolar concentrations (IC50=24 nM for Wee1 and 72 nM for Myt1). This compound is also a novel G2 checkpoint abrogator. It induces apoptosis.
iScience, 2025, 28(5):112292
Signal Transduct Target Ther, 2024, 9(1):181.
Nat Commun, 2024, 15(1):2089
S9639 Gartisertib (M4344, VX-803) VX-803 (M4344, ATR inhibitor 2) is an ATP-competitive, orally active, and selective inhibitor of ataxia telangiectasia and Rad3 related (ATR) kinase with Ki of < 150 pM. VX-803 (M4344) potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (P-Chk1) phosphorylation with IC50 of 8 nM. VX-803 (M4344) exhibits potential antineoplastic activity.
Mol Syst Biol, 2025, 21(3):231-253
iScience, 2025, 28(3):111943
Nat Biomed Eng, 2024, 10.1038/s41551-024-01277-5
S6740 DB07268 DB07268 is a potent and selective JNK1 inhibitor with an IC50 value of 9 nM and exhibits at least 70- to 90-fold greater potency against JNK1 than CHK1, CK2, and PLK.