SB-415286

Glycogen synthase kinase 3 (GSK3) is a serine/threonine protein kinase that is inhibited by an assortment of extracellular stimuli such as insulin, growth factors, cell specification factors, and cell adhesion. Its activity regulates many cell functions including the control of cell division, apoptosis, and inflammation. SB-415286 is a potent and selective cell-permeable, ATP-competitive inhibitor of GSK3? with an IC50 value of 78 nM (similar potency for GSK3?) and a Ki value of 31 nM. {15623} 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.{15623} SB-415286 also protects primary neurons from death induced by the PI3-kinase pathway.{15622}