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CHIR-99021 is a cell-permeable, ATP-competitive inhibitor of GSK-3α/β (IC50 values of 10 nM and 6.7 nM against GSK-3α and GSK-3β, respectively). GSK-3α/β are serine/threonine kinase agonists of the Wnt/β-catenin signaling pathway; thus, CHIR-99021 functions as a potent activator of Wnt. CHIR-99021 exhibits high selectivity for GSK-3α/β over closely related kinases (>500-fold), which include CDC2 and ERK2. As a modulator of Wnt signaling, CHIR-99021 has proved useful for cancer biology and is frequently used in stem cell research and regenerative medicine by inducing self-renewal and pluripotency of embryonic stem cells (ESCs) and induced pluripotent stem cells (iPSCs).
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Last modified: November 4, 2024
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