SB216763

SB216763 is a potent, selective, and cell permeable glycogen synthase kinase-3 (GSK-3) inhibitor. It competes with ATP and potently inhibits the activity alpha and beta isozymes of GSK-3. GSK-3 is a serine/threonine protein kinase that is inhibited by an assortment of extracellular stimuli including insulin, growth factors, cell specification factors, and cell adhesion. SB216763 protects both central and peripheral nervous system neurones in culture from death induced by reduced PI 3-kinase pathway activity. Treatment of primary neural progenitor cells with SB216763 resulted in an increase in the percentage of TuJ1-positive immature neurons, suggesting an inhibitory role of GSK3 in embryonic neurogenesis. It stimulates glycogen synthesis in Chang human liver cells. SB216763 treatment reduces cell viability in a dose-dependent manner, and leads to significant increase in apoptosis due to the specific down regulation of GSK-3 beta.