487021-52-3|AR-A014418|CsnPharm

CAS No.: 487021-52-3

AR-A014418 Catalog No. CSN15984

Synonyms: AR 0133418;GSK 3β inhibitor VIII;AR 014418

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

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实验方案

技术信息

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].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
human BxPC3 cells	-	Growth inhibition assay	72 h	Growth inhibition of human BxPC3 cells after 72 hrs by MTS assay, IC50=14 μM	19338355
human HUPT3 cells	-	Growth inhibition assay	72 h	Growth inhibition of human HUPT3 cells after 72 hrs by MTS assay, IC50=22 μM	19338355
human MIAPaCa2 cells	-	Growth inhibition assay	72 h	Growth inhibition of human MIAPaCa2 cells after 72 hrs by MTS assay, IC50=29 μM	19338355

参考文献

[1] Carter YM, Kunnimalaiyaan S, et al. Specific glycogen synthase kinase-3 inhibition reduces neuroendocrine markers and suppresses neuroblastoma cell growth. Cancer Biol Ther. 2014 May;15(5):510-5.
[2] Bhat R, Xue Y, et al. Structural insights and biological effects of glycogen synthase kinase 3-specific inhibitor AR-A014418. J Biol Chem. 2003 Nov 14;278(46):45937-45.
[3] Bhat R, Xue Y, Berg S, et al. Structural insights and biological effects of glycogen synthase kinase 3-specific inhibitor AR-A014418. J Biol Chem. 2003;278(46):45937-45945.
[4] Koh SH, Kim Y, Kim HY, Hwang S, Lee CH, Kim SH. Inhibition of glycogen synthase kinase-3 suppresses the onset of symptoms and disease progression of G93A-SOD1 mouse model of ALS. Exp Neurol. 2007;205(2):336-346.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.2435 mL
- 16.2173 mL
- 32.4346 mL
- 5 mM
- 0.6487 mL
- 3.2435 mL
- 6.4869 mL
- 10 mM
- 0.3243 mL
- 1.6217 mL
- 3.2435 mL

技术信息

CAS号

487021-52-3

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C12H12N4O4S

运输

蓝冰

分子量

308.31

别名

AR 0133418;GSK 3β inhibitor VIII;AR 014418;GSK-3beta Inhibitor VIII;Glycogen Synthase Kinase 3β Inhibitor VIII;SN-4521;AR-AO-14418

溶解度

DMSO	61.0 mg/mL (197.9 mM)
Water	Insoluble
Ethanol	Insoluble

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