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Characteristics
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A cell-permeable, potent, and ATP-competitive inhibitor of Chk2 (checkpoint kinase 2, IC50 = 15 nM, Ki = 37 nM). Displays approx. 1,000-fold greater selectivity for Chk2 compared to cdk1/cyclin B and CK1 (IC50 = 12 µM and 17 µM, respectively) and only weakly affects the activities of a panel of 31 kinases (< 25 % inhibition at 10 µM), including Chk1. Shown to rescue both peripheral CD4+ and CD8+ T-cells from gamma-irradiation-induced apoptosis with an EC50 of 3 µM and 7.6 µM, respectively.
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