SB 415286 is a potent and selective cell-permeable, ATP-competitive GSK3α inhibitor with an IC50 and a Ki of 78 and 31 nM, respectively. SB 415286 competes with ATP. SB 415286 has minimal activity against 24 other protein kinases （IC50 > 10 μ M）. SB 415286 stimulates glycogen synthesis, gene transcription and is neuroprotective. As a result of GSK3 inhibition, SB 415286 stimulates glycogen synthesis in the Chang human liver cell line with an EC50 value of 2.9 µM. SB 415286 also protects primary neurons from death induced by the PI3-kinase pathway. In L6 myotubes, SB 415286 induced a much greater activation of GS （6.8-fold） . In adipocytes, SB 415286 caused a comparable activation of GS despite a substantial differentiation-linked reduction in GSK3 expression （ approximay 85%） indicating that GSK3 remains an important determinant of GS activation in fat cells. ^[1] SB 415286 induced expression of a beta-catenin-LEF/TCF regulated reporter gene in HEK293 cells. ^[2]

• Use of lithium and SB-415286 to explore the role of glycogen synthase kinase-3 in the regulation of glucose transport and glycogen synthase. MacAulay K et al. Eur J Biochem 2003 Sep;270（18）:3829-38
• Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription. Coghlan MP et al. Chem Biol 2000 Oct;7（10）:793-803