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GSK-3βInhibitor II
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GSK-3βInhibitor II图片
CAS NO:478482-75-6
规格:98%
分子量:395.2
包装与价格:
包装价格(元)
5mg电议
10mg电议

产品介绍
GSK-3β inhibitor
CAS:478482-75-6
分子式:C14H10IN3OS
分子量:395.2
纯度:98%
存储:Store at -20°C

Background:

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.


Clinical trial: So far, no clinical study has been conducted.


参考文献:
[1] Naerum, L. ,Nrskov-Lauritsen, L. and Olesen, P.H. Scaffold hopping and optimization towards libraries of glycogen synthase kinase-3 inhibitors. Bioorg.Med.Chem.Lett. 12(11), 1525-1528 (2002).
[2] Watcharasit, P. ,Bijur, G.N.,Song, L., et al. Glycogen synthase kinase-3beta (GSK3beta) binds to and promotes the actions of p53. J.Biol.Chem. 278(49), 49972-48879 (2003).