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AR-A014418

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Chemical Structure| 487021-52-3 同义名 : GSK 3β inhibitor VIII;AR 0133418;GSK-3beta Inhibitor VIII.;AR-AO-14418;SN 4521;Glycogen Synthase Kinase 3β Inhibitor VIII;AR 014418
CAS号 : 487021-52-3
货号 : A174426
分子式 : C12H12N4O4S
纯度 : 99%+
分子量 : 308.313
MDL号 : MFCD08277040
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(340.56 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • GSK-3β

    GSK-3β, Ki:38 nM
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 (Ki=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
细胞系 浓度 检测类型 检测时间 活动说明 数据源
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
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.24mL

0.65mL

0.32mL

16.22mL

3.24mL

1.62mL

32.43mL

6.49mL

3.24mL
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.