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GlaxoSmithKline
Chemical Name:3-[(3-Chloro-4-hydroxyphenyl)amino]-4-(2-nitrophenyl)-1
H-pyrrole-2,5-dione
Biological Activity:
Potent and selective glycogen
synthase kinase-3 (GSK-3) inhibitor (Ki = 31 nM for GSK-3α);
competes with ATP. Has minimal activity against 24 other protein kinases (IC50
> 10 μM). Stimulates glycogen synthesis, gene transcription and is
neuroprotective.
Coghlanet al (2000) Selective small molecule inhibitors of
glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription.
Chem.Biol. 7
793. Crosset al (2001) Selective small-molecule inhibitors of
glycogen synthase kinase-3 activity protect primary neurones from death.
J.Neurochem. 77 94. Liang and Chuang (2006) Regulation and
function of glycogen synthase kinase-3 isoforms in neuronal survival.
J.Biol.Chem. 282 3904.
