BRD3731

BRD3731 is a selective GSK3β inhibitor, with IC50s of 15 nM and 215 nM for GSK3β and GSK3α, respectively. BRD3731 can be used for the research of a mood disorder, post-traumatic stress disorder (PTSD), psychiatric disorder, diabetes, and neurodegenerative disorder[1].

Signaling Pathways >> Stem Cell/Wnt >> GSK-3

Research Areas >> Neurological Disease

Signaling Pathways >> PI3K/Akt/mTOR >> GSK-3

GSK-3β:15 nM (IC50)

GSK-3α:215 nM (IC50)

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 inHL-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]

BRD3731 (30 mg/kg; i.p.) reduces audiogenic seizures in Fmr1 KO mice[1].

[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.