GSK3 Inhibitor XIII

GSK3 Inhibitor XIII is an aminopyrazole ATP-competitive inhibitor of glycogen synthase kinase 3 (GSK3), with 34% inhibition when used at a concentration of 2.5 µM. It inhibits androgen receptor transactivation in 22Rv1, LNCaP, and LNCaP-SSR cell lines in a dose-dependent manner. It promotes nuclear export of the androgen receptor and decreases translocation to the nucleus in PC3 and PCa prostate cancer cells, respectively. In HEK293 cells expressing the rat Nav1.2 channel, pretreatment with GSK3 inhibitor XIII dose-dependently potentiates peak current densities.

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2: Schütz SV, Cronauer MV, Rinnab L. Inhibition of glycogen synthase kinase-3beta promotes nuclear export of the androgen receptor through a CRM1-dependent mechanism in prostate cancer cell lines. J Cell Biochem. 2010 Apr 15;109(6):1192-200. doi: 10.1002/jcb.22500. PubMed PMID: 20127713.