CHIR-98014

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Description

CHIR-98014 is a potent and selective human GSK-3 inhibitor for human GSK-3ɑ and human GSK-3β with IC50 of 0.65 and 0.58 nM, respectively. CHIR-98014 inhibits human GSK-3β with Ki values of 0.87 nM. Although CHIR-98014 serves as a simple competitive inhibitor of ATP binding, CHIR-98014 exhibits from 500-fold to <1000-fold selectivity for GSK-3 versus 20 other protein kinases including CDC2, erk2, tie2, KDR et al. CHIR-98014 prevents CDC2 with an IC50 of 3.7 μM.

Application

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