CAS:264218-23-7SB-415286

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SB-415286 is an ATP-competitive inhibitor of GSK3α/GSK3β with IC50 of 78 nM and Ki of 31 nM.

规格	价格	促销价格	库存

18817579266

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18817579266

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实验数据

技术信息

CAS号

264218-23-7

储存条件

分子式

C16H10ClN3O5

运输

蓝冰

分子量

359.72

别名

溶解度

DMSO	83.0 mg/mL (230.7 mM)
Water	insoluble

动物实验配方

生物活性

描述Glycogen synthase kinase-3 (GSK-3) is a serine/threonine protein kinase encoded by two highly homologous and ubiquitously expressed genes with ability to phosphorylate and inactivate glycogen synthase, the rate limiting enzyme in glycogen synthesis. SB-415286 is a potent and selective inhibitor of GSK-3 with IC₅₀s of 77.5 nM for both hGSK-3α and hGSK-3β and a K_i of 30.75 nM for hGSK-3α. In the Chang human liver cell line, SB-415286 stimulated glycogen synthase activity thus promoting glycogen synthesis with EC₅₀ of 2.9 μM. Using a HEK293 transient transfection β-catenin-LEF/TCF luciferase reporter assay, SB-415286 dose-dependently induced transcription of the β-catenin dependent gene^[3]. SB-415286 (25, 50 and 100 μM; 24, 48, 72 and 96 h) showed anti-proliferative effect in Neuro-2a, SK-N-SH and SK-N-BE cell lines in a dose and time dependent manner. In vivo, daily i.p. injections of SB-415286 produced a significant tumor growth delay in the tumor-bearing mice^[4].