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 GSK3α with an IC50 value of 78 nM (similar potency for GSK3β) and a Ki value of 31 nM. 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.
SB 415286 was used to treat neuroblastoma cells and study the effect of GSK-3 inhibition on cell proliferation.
ChEBI: A member of the class of maleimides carrying 3-chloro-4-hydroxyphenylamino and 2-nitrophenyl substituents at positions 3 and 4 respectively.
Potent and selective glycogen synthase kinase-3 (GSK-3) inhibitor (K i = 31 nM for GSK-3 α ); competes with ATP. Has minimal activity against 24 other protein kinases (IC 50 > 10 μ M). Stimulates glycogen synthesis, gene transcription and is neuroprotective.
SB 415286 is a small molecule inhibitor of GSK-3 in muscle and fat cells. SB 415286 induces activation of glycogen synthase and regulates the transport glucose. SB 415286 reduces the systemic inflammation induced by endotoxic shock in rat model of acute colitis. It increases the axonal growth and promotes the recovery of injured adult CNS neurons. SB 415289 is implicated in inducing chromosome instability when used as therapeutic agents.
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