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Description

A cell-permeable, potent, reversible and ATP-competitive inhibitor of Chk2 (checkpoint kinase 2, IC50 = 15 nM, Ki = 37 nM). Displays ~1,000-fold greater selectivity for Chk2 compared to Cdk1/cyclin B and CK1 (IC50 = 12 µ,M and 17 µ,M, respectively) and only weakly affects the activities of a panel of 31 kinases (<25% inhibition at 10 µ,M), including Chk1. Shown to rescue both peripheral CD4+ and CD8+ T-cells from gamma-irradiation-induced apoptosis with an EC50 of 3 µ,M and 7.6 µ,M, respectively., A cell-permeable and reversible benzimidazolo compound that acts as a potent and ATP-competitive inhibitor of Chk2 with an IC50 of 15 nM and a Ki of 37 nM. Displays ~ 1,000-fold greater selectivity over Cdk1/B and CK1 (IC50 = 12 M and 17 M, respectively) and only weakly affects the activities of a panel of 31 kinases (<25% inhibition at 10 M), including Chk1. Shown to rescue both peripheral CD4+ and CD8+ T-cells from gamma-irradiation-induced apoptosis with an EC50 of 3 M and 7.6 M, respectively. Also available as a 25 mM solution in DMSO (Cat. No. 220491).