5H-Pyrazolo[3,4-b]quinolin-5-one, 3-(2,2-dimethylpropyl)-1,2,4,6,7,8-hexahydro-4,7,7-trimethyl-4-phenyl-, (4S)-

Biological Activity

BRD3731 is a selective GSK3β inhibitor, with IC50s of 15 nM and 215 nM for GSK3β and GSK3α, respectively. BRD3731 is potentail for the research of post-traumatic stress disorder (PTSD), psychiatric disorder, diabetes, and neurodegenerative disorders[1]. BRD3731 is a GSK3β- selective inhibitor extracted from patent US20160375006A1, compound example 272[1].BRD3731 (1-10 μM; 24 hours) inhibits the phosphorylation of CRMP2 in SH-SY5Y cells[1].BRD3731 (20 μM; 24 hours) decreases β-catenin S33/37/T41 phosphorylation and induces β-catenin S675 phosphorylation in HL-60 cells[2].BRD3731 (10-20 μM; 7-10 days) impairs colony formation in TF-1 and increases colony forming ability in the MV4-11 cell line[2]

References

[1]. Edward Scolnick, et al. Uses of paralog-selective inhibitors of gsk3 kinases. US20160375006A1. [2]. Wagner FF, et, al. Exploiting an Asp-Glu "switch" in glycogen synthase kinase 3 to design paralog-selective inhibitors for use in acute myeloid leukemia. Sci Transl Med. 2018 Mar 7;10(431):eaam8460.