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Overview
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Background
CHIR 99021 trihydrochloride is hydrochloride of CHIR 99021, which inhibits GSK-3α and GSK-3β with IC50 values of 10 nM and 6.7 nM. GSK-3 is a serine/threonine kinase, responsible for phosphorylating either the serine or threonine residues of its substrates. This phosphorylation process is involved in various key biological processes, including gene transcription, protein synthesis, cell signaling, cellular transport, proliferation, apoptosis, intracellular communication and glucose regulation.
1. Ring DB, Johnson KW, Henriksen EJ, et al. Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo. Diabetes, 2003, 52(3): 588-595.
2. Pandey MK, DeGrado TR. Glycogen synthase kinase-3 (GSK-3)-targeted therapy and imaging. Theranostics, 2016, 6(4): 571-593.
3. Mussmann R, Geese M, Harder F, et al. Inhibition of GSK3 promotes replication and survival of pancreatic beta cells. Journal of Biological Chemistry, 2007, 282(16): 12030-12037.
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Overview