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IC50: 390 nM for GSK-3β

GSK-3β Inhibitor II is a GSK-3β inhibitor.

Glycogen Synthase Kinase-3 (GSK-3), a protein-serine kinase, is implicated in the hormonal control of various regulatory proteins. A number of substrates have been identified, which implicates GSK-3 in the regulation of several physiological processes. Moreover, it has been reported that compounds that specifically inhibit GSK-3 activity may be useful in the treatment of diabetes.

In vitro: In a previous study, by using a virtual screening strategy based on a methodology derived from the CATS molecular descriptor, a novel compound class including GSK-3β Inhibitor II with inhibitory activity against the GSK-3 enzyme was identified via scaffold hopping. GSK-3β Inhibitor II was found to be a potent inhibitor of GSK-3β with the IC50 value of 390 nM. However, GSK-3β Inhibitor II was not able to inhibit another GSK-3 isoform, GSK-3α [1]. Another study found that GSK-3β Inhibitor II could block the functional regulation of p53 through inhibiting GSK-3β, decreasing MDM2 levels, and modulating mitochondrial p53 apoptotic signaling [2].

In vivo: Up to now, there is no animal in vivo data reported.

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