sb415286

Description: SB415286 is a novel, potent, selective, cell permeable and ATP-competitive GSK3alpha (glycogen synthase kinase-3alpha) inhibitor with potential anti-inflammatory activity. It inhibits GSK3alpha with an IC50/Ki of 78 nM/31 nM and has equal inhibitory against GSK-3beta. SB-415286 inhibited GSK-3 activity and promoted glycogen synthesis in human liver cells and induced expression of reporter gene regulated by catenin-LEF/TCF in HEK293 cells. In primary neurons, it can prevent cell death induced by repressed PI3k pathway activity. Further studies showed that reduced GSK3beta activity induced by SB-415286 could inhibit down-regulation of cyclin D1, cell cycle arrest and chemosensitivity, which were all mediated by rapamycin. Glycogen synthase kinase-3beta (GSK-3beta) is a multifunctional serine/threonine kinase that plays important roles in the necrosis and apoptosis of cardiomyocytes.

References: Chem Biol. 2000 Oct; 7(10):793-803; J Neurooncol. 2011 Aug; 104(1):145-53.