CAS:487021-52-3AR-A014418

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Synonyms: GSK-3β Inhibitor VIII;GSK-3beta Inhibitor VIII

AR-A014418 is a selective inhibitor of GSK3β with IC50 of 104 ± 27 nM.

规格	价格	促销价格	库存

18817579266

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18817579266

立即询价

实验数据

技术信息

CAS号

487021-52-3

储存条件

分子式

C12H12N4O4S

运输

蓝冰

分子量

308.31

别名

GSK-3β Inhibitor VIII;GSK-3beta Inhibitor VIII

溶解度

动物实验配方

生物活性

靶点 GSK-3β

IC50:104+/-27nM
描述Glycogen synthase kinase 3 (GSK3) is a serine/threonine kinase involved in the pathogenesis of diabetes and Alzheimer's disease. AR-A014418 is a GSK3 inhibitor with an IC50 value of 104±27nM. It inhibits GSK3 in an ATP-competitive manner (K_i=38nM). In 3T3 fibroblasts stably expressing four-repeat tau protein, AR-A014418 (100nM-50μM) inhibited tau phosphorylation in a dose-dependent manner with an IC50 of 2.7μM. AR-A014418 also protected neuroblastoma N2A cells from death induced by reduced PI3K pathway activity in a dose-dependent manner with an IC50 of 0.5μM^[3]. Intraperitoneal injection of JNJ-63533054 (1-4μg/g) dose-dependently delayed the onset of symptoms, slowed down disease progression, and inhibited the activity of GSK-3 in an amyotrophic lateral sclerosis mouse model harboring the G93A mutant human SOD1 gene^[4].
作用机制AR-A014418 is a thiazole that inhibits GSK3 in an ATP-competitive manner^[3].