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Chk Signaling Pathway Map

Isoform-selective Inhibitors

Chk Products

All (15)
Chk Inhibitors (14)
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New Chk Products

Catalog No.	Product Name	Information	Product Use Citations
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.	Sci Adv, 2021, 7(25)eabd9208 Leukemia, 2021, 10.1038/s41375-021-01347-6 Theranostics, 2021, 11(4):1795-1813
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 Genet, 2021, 10.1038/s41588-021-00893-0 Cancer Cell, 2021, S1535-6108(21)00383-4 Nucleic Acids Res, 2021, gkab643
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.	Nucleic Acids Res, 2020, 24;gkaa268 Cell Rep, 2020, 32(9):108080 mBio, 2020, 11(1)
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.	Nat Genet, 2021, 10.1038/s41588-021-00893-0 Mol Cell, 2021, 81(19):4041-4058.e15 Nat Commun, 2021, 12(1):6667
S2904	PF-477736	PF-477736 (PF-736, PF-00477736) is a selective, potent and ATP-competitive Chk1 inhibitor with K_i 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. Phase 1.	FEBS J, 2021, 10.1111/febs.15747 DNA Repair (Amst), 2021, 101:103099 Cell Rep, 2020, 32(12):108184
S6385^New	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, 2021, 184(25):6119-6137.e26 ACS Pharmacol Transl Sci, 2021, 4(4):1449-1461
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.
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.	Nucleic Acids Res, 2021, gkab628 Leukemia, 2021, 10.1038/s41375-021-01347-6 Leukemia, 2021, 10.1038/s41375-021-01361-8
S7740	SAR-020106	SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC50 of 13.3 nM.
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.	Cancer Sci, 2020, 112(1):133-143 Nature, 2019, 10.1038/s41586-019-1607-3 Nature, 2019, 574(7777):268-272
S8253	CCT245737	CCT245737 (SRA737, PNT-737) is an orally active CHK1 inhibitor with The IC50 of 1.4 nM. It exhibits >1,000-fold selectivity against CHK2 and CDK1.	Mol Cancer, 2021, 20(1):97 Oncogene, 2021, 10.1038/s41388-021-02080-1 Cancer Discov, 2020, CD-20-0581
S8526	GDC-0575 (ARRY-575)	GDC-0575 (ARRY-575, RG7741) is a potent and selective CHK1 inhibitor with an IC50 of 1.2 nM.	Biochem Biophys Res Commun, 2021, 584:7-14 J Clin Invest, 2020, 139080 Life Sci Alliance, 2020, 3(8):e202000671
S8632	Chk2 Inhibitor II (BML-277)	Chk2 Inhibitor II (BML-277) 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.	Mol Cancer Res, 2021, 10.1158/1541-7786.MCR-20-0791 mBio, 2020, 11(3):e01190-20 BMC Cancer, 2020, 20(1):4
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.
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.
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.	Sci Adv, 2021, 7(25)eabd9208 Leukemia, 2021, 10.1038/s41375-021-01347-6 Theranostics, 2021, 11(4):1795-1813
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 Genet, 2021, 10.1038/s41588-021-00893-0 Cancer Cell, 2021, S1535-6108(21)00383-4 Nucleic Acids Res, 2021, gkab643
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.	Nucleic Acids Res, 2020, 24;gkaa268 Cell Rep, 2020, 32(9):108080 mBio, 2020, 11(1)
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.	Nat Genet, 2021, 10.1038/s41588-021-00893-0 Mol Cell, 2021, 81(19):4041-4058.e15 Nat Commun, 2021, 12(1):6667
S2904	PF-477736	PF-477736 (PF-736, PF-00477736) is a selective, potent and ATP-competitive Chk1 inhibitor with K_i 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. Phase 1.	FEBS J, 2021, 10.1111/febs.15747 DNA Repair (Amst), 2021, 101:103099 Cell Rep, 2020, 32(12):108184
S6385^New	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, 2021, 184(25):6119-6137.e26 ACS Pharmacol Transl Sci, 2021, 4(4):1449-1461
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.
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.	Nucleic Acids Res, 2021, gkab628 Leukemia, 2021, 10.1038/s41375-021-01347-6 Leukemia, 2021, 10.1038/s41375-021-01361-8
S7740	SAR-020106	SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC50 of 13.3 nM.
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.	Cancer Sci, 2020, 112(1):133-143 Nature, 2019, 10.1038/s41586-019-1607-3 Nature, 2019, 574(7777):268-272
S8253	CCT245737	CCT245737 (SRA737, PNT-737) is an orally active CHK1 inhibitor with The IC50 of 1.4 nM. It exhibits >1,000-fold selectivity against CHK2 and CDK1.	Mol Cancer, 2021, 20(1):97 Oncogene, 2021, 10.1038/s41388-021-02080-1 Cancer Discov, 2020, CD-20-0581
S8526	GDC-0575 (ARRY-575)	GDC-0575 (ARRY-575, RG7741) is a potent and selective CHK1 inhibitor with an IC50 of 1.2 nM.	Biochem Biophys Res Commun, 2021, 584:7-14 J Clin Invest, 2020, 139080 Life Sci Alliance, 2020, 3(8):e202000671
S8632	Chk2 Inhibitor II (BML-277)	Chk2 Inhibitor II (BML-277) 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.	Mol Cancer Res, 2021, 10.1158/1541-7786.MCR-20-0791 mBio, 2020, 11(3):e01190-20 BMC Cancer, 2020, 20(1):4
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.
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.
S6385^New	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, 2021, 184(25):6119-6137.e26 ACS Pharmacol Transl Sci, 2021, 4(4):1449-1461