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Potent and selective cell permeable, ATP-competitive inhibitor of GSK3α with an IC50 value of 78nM (and similar potency for GSK3β).
DYRK1A inhibitor (IC50=0.9µM).
Stimulates glycogen synthesis in liver cells and induces β-catenin-dependent gene transcription.
Acts as neuroprotectant and prevents neuronal cell death induced by PI3-kinase pathway.
Anticancer agent with antiproliferative activity.
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.
Product References
Selective small molecule inhibitors or glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription: M.P. Coghlan, et al.; Chem. & Biol. 7, 793 (2000)
Selective small-molecule inhibitors of glycogen synthase kinase-3 activity protect primary neurons from death: D.A.E. Cross, et al.; J. Neurochem. 77, 94 (2001)
Use of lithium and SB-415286 to explore the role of glycogen synthase kinase-3 in the regulation of glucose transport and glycogen synthase: K. MacAulay, et al.; Eur. J. Biochem. 270, 3829 (2003)
GSK3 inhibitors: development and therapeutic potential: P. Cohen & M. Goedert; Nat. Rev. Drug Discov. 3, 479 (2004)
Reduction of experimental colitis in the rat by inhibitors of glycogen synthase kinase-3beta: B.J.R. Whittle, et al.; Br. J. Pharmacol. 147, 575 (2006)
The selectivity of protein kinase inhibitors: a further update: J. Bain, et al.; Biochem. J. 408, 297 (2007)
Inactivation of glycogen synthase kinase 3 promotes axonal growth and recovery in the CNS: J. Dill, et al.; J. Neurosci. 28, 8914 (2008)
A molecular study of pathways involved in the inhibition of cell proliferation in neuroblastoma B65 cells by the GSK-3 inhibitors lithium and SB-415286: J.G. Pizarro, et al.; J. Cell. Mol. Med. 13, 3906 (2009)
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