Chk

Isoform-selective Products

Signaling Pathway

Chk Signaling Pathway

Chk Products

  • All (16)
  • Chk Inhibitors (15)
  • Chk Activator (1)
  • New Chk Products
Catalog 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.
Pharmacol Res, 2024, 201:107091
Mol Cell, 2023, 83(5):803-818.e8
EMBO Mol Med, 2023, e16431.
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.
bioRxiv, 2024, 2024.02.06.579216
Nat Commun, 2023, 14(1):6088
Nat Commun, 2023, 14(1):4991
S2735 MK-8776 (SCH 900776) MK-8776 (SCH 900776) is a selective Chk1 inhibitor with IC50 of 3 nM in a cell-free assay. It shows 500-fold selectivity against Chk2. Phase 2.
Pharmacol Res, 2024, 201:107091
Viruses, 2024, 16(2)282
Cell Rep, 2023, 42(7):112792
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, 2023, S2211-1247(23)00490-4
NPJ Regen Med, 2023, 8(1):20
npj Regenerative Medicine, 2023, 20-2023)
S7178 Prexasertib HCl (LY2606368) 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.
Viruses, 2024, 16(2)282
EMBO Mol Med, 2023, e16431.
Cell Death Discov, 2023, 9(1):285
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.
Nat Commun, 2023, 14(1):6088
Cell Death Discov, 2023, 9(1):313
Cells, 2023, 12(10)1387
S8632 BML-277 (Chk2 Inhibitor II) BML-277 (Chk2 Inhibitor II) is an ATP-competitive inhibitor of Chk2 with IC50 of 15 nM. It is 1000-fold more selective toward Chk2 serine/threonine kinase than for Chk1 and Cdk1/B kinases. Chk2 Inhibitor II (BML-277) dose dependently protects human CD4(+) and CD8(+) T-cells from apoptosis due to ionizing radiation.
Nat Commun, 2023, 14(1):6088
iScience, 2023, 26(7):107090
Cancers (Basel), 2023, 15(15)3987
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.

EMBO Mol Med, 2023, e16431.
EBioMedicine, 2023, 95:104752
J Biol Chem, 2023, S0021-9258(23)01969-5
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.
Mol Oncol, 2023, 10.1002/1878-0261.13537
Biochem J, 2022, 479(19):2063-2086
Mol Cancer, 2021, 20(1):97
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
Front Cardiovasc Med, 2023, 10:1187490
J Exp Clin Cancer Res, 2022, 41(1):141
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). PD0166285 is also a novel G2 checkpoint abrogator. PD0166285 induces apoptosis.
Nat Commun, 2023, 14(1):6088
Cancer Sci, 2020, 112(1):133-143
Nature, 2019, 10.1038/s41586-019-1607-3
S9639 VX-803 (M4344) 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.
bioRxiv, 2024,
Viruses, 2023, 15(5)1112
NAR Cancer, 2023, 5(1):zcac045
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.
S3224 Cinobufagin Cinobufagin (Cinobufagine), an active ingredient of Venenum Bufonis, inhibits tumor development. Cinobufagin increases ATM and Chk2 and decreases CDC25C, CDK1, and cyclin B. Cinobufagin inhibits PI3K, AKT and Bcl-2 while increases levels of cleaved caspase-9 and caspase-3. Thus, Cinobufagin induces cell cycle arrest at the G2/M phase and apoptosis.
S7740 SAR-020106 SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC50 of 13.3 nM.
E1667New LY2880070 LY2880070 is an orally active inhibitor of CHK1. LY2880070 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.
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.
Pharmacol Res, 2024, 201:107091
Mol Cell, 2023, 83(5):803-818.e8
EMBO Mol Med, 2023, e16431.
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.
bioRxiv, 2024, 2024.02.06.579216
Nat Commun, 2023, 14(1):6088
Nat Commun, 2023, 14(1):4991
S2735 MK-8776 (SCH 900776) MK-8776 (SCH 900776) is a selective Chk1 inhibitor with IC50 of 3 nM in a cell-free assay. It shows 500-fold selectivity against Chk2. Phase 2.
Pharmacol Res, 2024, 201:107091
Viruses, 2024, 16(2)282
Cell Rep, 2023, 42(7):112792
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, 2023, S2211-1247(23)00490-4
NPJ Regen Med, 2023, 8(1):20
npj Regenerative Medicine, 2023, 20-2023)
S7178 Prexasertib HCl (LY2606368) 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.
Viruses, 2024, 16(2)282
EMBO Mol Med, 2023, e16431.
Cell Death Discov, 2023, 9(1):285
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.
Nat Commun, 2023, 14(1):6088
Cell Death Discov, 2023, 9(1):313
Cells, 2023, 12(10)1387
S8632 BML-277 (Chk2 Inhibitor II) BML-277 (Chk2 Inhibitor II) is an ATP-competitive inhibitor of Chk2 with IC50 of 15 nM. It is 1000-fold more selective toward Chk2 serine/threonine kinase than for Chk1 and Cdk1/B kinases. Chk2 Inhibitor II (BML-277) dose dependently protects human CD4(+) and CD8(+) T-cells from apoptosis due to ionizing radiation.
Nat Commun, 2023, 14(1):6088
iScience, 2023, 26(7):107090
Cancers (Basel), 2023, 15(15)3987
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.

EMBO Mol Med, 2023, e16431.
EBioMedicine, 2023, 95:104752
J Biol Chem, 2023, S0021-9258(23)01969-5
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.
Mol Oncol, 2023, 10.1002/1878-0261.13537
Biochem J, 2022, 479(19):2063-2086
Mol Cancer, 2021, 20(1):97
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
Front Cardiovasc Med, 2023, 10:1187490
J Exp Clin Cancer Res, 2022, 41(1):141
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). PD0166285 is also a novel G2 checkpoint abrogator. PD0166285 induces apoptosis.
Nat Commun, 2023, 14(1):6088
Cancer Sci, 2020, 112(1):133-143
Nature, 2019, 10.1038/s41586-019-1607-3
S9639 VX-803 (M4344) 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.
bioRxiv, 2024,
Viruses, 2023, 15(5)1112
NAR Cancer, 2023, 5(1):zcac045
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.
S7740 SAR-020106 SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC50 of 13.3 nM.
E1667New LY2880070 LY2880070 is an orally active inhibitor of CHK1. LY2880070 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.
S3224 Cinobufagin Cinobufagin (Cinobufagine), an active ingredient of Venenum Bufonis, inhibits tumor development. Cinobufagin increases ATM and Chk2 and decreases CDC25C, CDK1, and cyclin B. Cinobufagin inhibits PI3K, AKT and Bcl-2 while increases levels of cleaved caspase-9 and caspase-3. Thus, Cinobufagin induces cell cycle arrest at the G2/M phase and apoptosis.
E1667New LY2880070 LY2880070 is an orally active inhibitor of CHK1. LY2880070 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.

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Tags: Checkpoint activation | Checkpoint kinase | Checkpoint function | Checkpoint activity | Chk1 phosphorylation | Checkpoint pathway | Chk1 pathway | Chk2 pathway | Chk2 phosphorylation | Chk1 inhibitor clinical trial | Chk1 inhibition | Chk1 activation | Chk2 activation | Chk1 assay | Chk inhibitors review