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Home > Inhibitors & Agonists > Cell Cycle/DNA Damage > Checkpoint Kinase (Chk)

Checkpoint Kinase (Chk)

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Cat. No. Product Name Field of Application Chemical Structure
DC10796 Prexasertib (LY2606368) Featured
LY2606368 is a potent and selective ATP competitive inhibitor(IC50=1.5 nM in SW1990 cell) of the Chk1 protein kinase.
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DC74584 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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DC7076 AZD-7762 Featured
AZD7762 is a potent and selective inhibitor of Chk1 with IC50 of 5 nM; equally potent against Chk2 and less potent against CAM, Yes, Fyn, Lyn, Hck and Lck.
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DC5024 MK-8776 (SCH 900776) Featured
SCH 900776 is a selective Chk1 inhibitor with IC50 of 3 nM. It shows 50-fold selectivity against Chk2. Phase 2.
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DC7993 Prexasertib (LY2606368) 2HCl Featured
LY2606368 2Hcl is a potent and selective ATP competitive inhibitor(IC50=1.5 nM in SW1990 cell) of the Chk1 protein kinase.
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DC7103 LY2603618(IC-83) Featured
LY2603618(IC-83) is a potent and selective small molecule inhibitor of Chk1 protein kinase activity in vitro (IC50=7 nM) and the first selective Chk1 inhibitor to enter clinical cancer trials.
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DC9792 SAR020106 Featured
SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC(50) of 13.3 nmol/L on the isolated human enzyme.
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DC8259 PF0477736 Featured
PF 477736 is a CHK inhitor with Ki values of 0.49 and 47 nM for Chk1 and Chk2 respectively. A proprietary compound targeting cell cycle checkpoint kinase 1 (chk1) with potential chemopotentiation activity
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DC8324 CCT244747 Featured
CCT244747 represents the first structural disclosure of a highly selective, orally active CHK1 inhibitor and warrants further evaluation alone or combined with genotoxic anticancer therapies.
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DC48120 Chk1-IN-6
Chk1-IN-6 is a potent, selective, and orally bioavailable CHK1 inhibitor candidate.
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DC10485 GDC0575(ARRY-575,RG7441) Featured
GDC0575(ARRY-575,RG7441)is a small molecule inhibitor of cell cycle checkpoint kinase 1 (Chk1), with potential chemosensitization activity.
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DC41105 Prexasertib dimesylate
Prexasertib dimesylate (LY2606368 dimesylate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib dimesylate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib dimesylate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dimesylate shows potent anti-tumor activity.
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DC41104 Prexasertib Mesylate Hydrate
Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib Mesylate Hydrate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib Mesylate Hydrate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib Mesylate Hydrate shows potent anti-tumor activity.
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DC40569 Chk1-IN-5
Chk1-IN-5 is a potent checkpoint kinase 1 (Chk1) inhibitor. Chk1-IN-5 inhibits Chk1 phosphorylation and inhibits tumor growth in colon cancer xenograft model.
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DC9924 SB218078 Featured
SB218078 is an inhibitor of checkpoint kinase 1 (Chk1) that displays selectivity over other protein kinases (IC50 values are 15, 250 and 1000 nM for Chk1, cdc2 and PKC respectively).
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DC11732 GNE-900
GNE-900 (GNE900) is a potent, selective, ATP-competitive, and orally bioavailable Chk1 inhibitor with IC50 of <1 nM.
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DC9399 CCT241533 (hydrochloride)
CCT241533 Hcl is a potent serine/threonine checkpoint kinase (Chk2) inhibitor with IC50 of 3 nM; shows minimal cross-reactivity against a panel of kinases at 1 uM.
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DC11716 XL-844
A potent, specific, orally available, ATP‑competitive inhibitor of Chk1 and Chk2 with Ki of 2.2 nM and 0.07 nM, respectively.
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DC11713 NSC-109555 ditosylate
A potent, selective, reversible, ATP-competitive Chk2 inhibitor with IC50 of 0.2 uM.
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DC11733 SAR-020106
A potent, selective, ATP-competitive Chk1 inhibitor with IC50 of 13.3 nM.
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DC11711 VER-158411
A potent, selective, ATP-competitive Chk1 and Chk2 inhibitor with IC50 of 4.4 nM and 4.5 nM, respectively.
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DC11710 GDC-0425
A potent, selective and orally active Chk1 inhibitor.
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DC11717 PD-321852
A potent, reasonably selective Chk1 inhibitor with cell IC50 of 5 nM.
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DC11714 PV-1019
A potent, ATP-competitive and highly selective Chk2 inhibitor with IC50 of 138 nM.
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DC11654 VRX-0466617
A potent and selective Chk2 inhibitor with Ki/IC50 of 11 nM/120 nM.
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DC11715 PV-1115
A potent and highly selective Chk2 inhibitor with IC50 of 0.14 nM.
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DC11953 MU 380
A novel potent, selective CHK1 inhibitor 2 nM, >80-fold selectivity over CHK2.
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DC11718 Debromohymenialdisine
A marine sponge alkaloid that inhibits Chk1 and Chk2 with IC50 of 3 and 3.5 uM, respectively.
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