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Chk

Isoform-selective Products

Chk1 Chk2

Signaling Pathway

Chk Products

All (17)
Chk Inhibitors (16)
Chk Activator (1)
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.	Mol Cell, 2024, S1097-2765(24)00285-5 Pharmacol Res, 2024, 201:107091 Cell Death Dis, 2024, 15(4):274
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.	Cell, 2024, 187(14):3652-3670.e40 Mol Cell, 2024, S1097-2765(24)00285-5 Neoplasia, 2024, 57:101038
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.	Acta Pharm Sin B, 2024, 14(6):2685-2697 EMBO J, 2024, 43(7):1301-1324 Cancer Lett, 2024, 592:216898
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.	Nature, 2024, 635(8037):210-218 Mol Cell, 2024, S1097-2765(24)00285-5 bioRxiv, 2024, 2024.06.24.600514
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.	Science, 2024, 384(6700):eadk0775 Mol Cancer, 2024, 23(1):242 Nat Commun, 2024, 15(1):2089
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.	Nat Commun, 2024, 15(1):8890 Cell Rep Med, 2024, 5(10):101778 Br J Cancer, 2024, 10.1038/s41416-024-02745-0
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.	bioRxiv, 2024, 2024.06.24.600514 Nat Commun, 2023, 14(1):6088 Nat Commun, 2023, 14(1):6088
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.	Nat Commun, 2024, 15(1):2089 Cell Death Dis, 2024, 15(4):274 Cell Death Discov, 2024, 10(1):278
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 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, 2024, 15(1):2089 medRxiv, 2024, 2023.05.17.23290140 Nat Commun, 2023, 14(1):6088
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.	Nat Biomed Eng, 2024, 10.1038/s41551-024-01277-5 bioRxiv, 2024, bioRxiv, 2024, 2024.06.24.600514
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.
E1653^New	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.
E1667^New	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.	Mol Cell, 2024, S1097-2765(24)00285-5 Pharmacol Res, 2024, 201:107091 Cell Death Dis, 2024, 15(4):274
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.	Cell, 2024, 187(14):3652-3670.e40 Mol Cell, 2024, S1097-2765(24)00285-5 Neoplasia, 2024, 57:101038
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.	Acta Pharm Sin B, 2024, 14(6):2685-2697 EMBO J, 2024, 43(7):1301-1324 Cancer Lett, 2024, 592:216898
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.	Nature, 2024, 635(8037):210-218 Mol Cell, 2024, S1097-2765(24)00285-5 bioRxiv, 2024, 2024.06.24.600514
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.	Science, 2024, 384(6700):eadk0775 Mol Cancer, 2024, 23(1):242 Nat Commun, 2024, 15(1):2089
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.	Nat Commun, 2024, 15(1):8890 Cell Rep Med, 2024, 5(10):101778 Br J Cancer, 2024, 10.1038/s41416-024-02745-0
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.	bioRxiv, 2024, 2024.06.24.600514 Nat Commun, 2023, 14(1):6088 Nat Commun, 2023, 14(1):6088
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.	Nat Commun, 2024, 15(1):2089 Cell Death Dis, 2024, 15(4):274 Cell Death Discov, 2024, 10(1):278
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 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, 2024, 15(1):2089 medRxiv, 2024, 2023.05.17.23290140 Nat Commun, 2023, 14(1):6088
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.	Nat Biomed Eng, 2024, 10.1038/s41551-024-01277-5 bioRxiv, 2024, bioRxiv, 2024, 2024.06.24.600514
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.
E1653^New	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.
E1667^New	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.
E1653^New	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.
E1667^New	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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