Chk2 Inhibitors

Catalog No. Product Name Information Selective / Pan IC50 / Ki
S1532 AZD7762

AZD7762 is a potent and selective inhibitor of Chk1 with IC50 of 5 nM. It is equally potent against Chk2 and less potent against CAM, Yes, Fyn, Lyn, Hck and Lck. Phase 1.

Pan Chk2, IC50: <10 nM
S2904 PF-477736

PF-477736 is a selective, potent and ATP-competitive Chk1 inhibitor with Ki of 0.49 nM and also inhibits VEGFR2, Aurora-A, FGFR3, Flt3, Fms (CSF1R), Ret and Yes. It shows ~100-fold selectivity for Chk1 than Chk2. Phase 1.

Pan Chk2, Ki: 47 nM
S2683 CHIR-124

CHIR-124 is a novel and potent Chk1 inhibitor with IC50 of 0.3 nM. It shows 2,000-fold selectivity against Chk2, 500- to 5,000-fold less activity against CDK2/4 and Cdc2.

Pan Chk2, IC50: 697.4 nM
S2735 MK-8776 (SCH 900776)

SCH 900776 is a selective Chk1 inhibitor with IC50 of 3 nM. It shows 500-fold selectivity against Chk2. Phase 2.

Pan Chk2, IC50: 1.5 μM