GSK-3 Inhibitor II is a potent inhibitor of GSK-3β (glycogen synthase kinase-3β) (IC|50|=390 nM). GSK-3 was first discovered to be involved in the control of glycogen metabolism, but has since been indicated in regulating a diverse range of cellular functions, such as neuronal cell survival and death. GSK-3β plays an important role in cardiomyopathies and has been shown to decrease MRP2 expression in neuronal growth factor (NGF)-induced PC-12 cells . Activation of GSK-3β plays a critical role in diabetes-related changes in cardiac energy metabolism, inflammation, nitrosative damage, and remodeling.
1.Naerum L, Nørskov-Lauritsen L, Olesen PH. (2002) Scaffold hopping and optimization towards libraries of glycogen synthase kinase-3 inhibitors.. Bioorg Med Chem Lett, 12 (11):(1525-8). [PMID:12031334][10.1021/op500134e]
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