2227279-84-5

GSK-3 inhibitor 3 is a selective, orally active and brain-penetrant inhibitor of GSK-3, with IC50s of 0.35 nM and 0.25 nM for GSK-3α and GSK-3β, respectively. GSK-3 inhibitor 3 lowers levels of tau protein phosphorylation at S396 in a triple-transgenic mouse Alzheimer’s disease model, with IC50 of 10 nM. GSK-3 inhibitor 3 can be used for neurological disease research[1].

GSK-3α: 0.35 nM (IC₅₀); GSK-3β: 0.25 nM (IC₅₀); CDK2: 0.22 μM (IC₅₀); CDK5: 1.3 μM (IC₅₀)

[1] Hartz RA, et.al. Discovery of 2-(Anilino)pyrimidine-4-carboxamides as Highly Potent, Selective, and Orally Active Glycogen Synthase Kinase-3 (GSK-3) Inhibitors. J Med Chem. 2023 Jun 8;66(11):7534-7552. DOI:10.1021/acs.jmedchem.3c00364