CAY10796 is an aminopyrazole ATP-competitive inhibitor of glycogen synthase kinase 3 (GSK3), with 34% inhibition when used at a concentration of 2.5 μM.
1 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.
1,2 In HEK293 cells expressing the rat Na
v1.2 channel, pretreatment with CAY10796 dose-dependently potentiates peak current densities.
3
1. Rinnab, L., Schütz, S.V., Diesch, J., et al. Inhibition of glycogen synthase kinase-3 in androgen-responsive prostate cancer cell lines: are GSK inhibitors therapeutically useful? Neoplasia 10(6),624-634(2008).
2. Schütz, S.V., Cronauer, M.V., and Rinnab, L. Inhibition of glycogen synthase kinase-3β promotes nuclear export of the androgen receptor through a CRM1-dependent mechanism in prostate cancer cell lines J. Cell. Biochem. 109(6),1192-1200(2010).
3. James, T.F., Nenov, M.N., Wildburger, N.C., et al. The Nav1.2 channel is regulated by GSK3 Biochim. Biophys. Acta 1850(4),832-844(2015).
