AR-A014418 | GSK 3β inhibitor VIII | GSK3β Inhibitor | AmBeed-信号通路专用抑制剂

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AR-A014418 99%+

货号：A174426 同义名： GSK 3β inhibitor VIII;AR 0133418

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

AR-A014418 化学结构
CAS号：487021-52-3

AR-A014418 3D分子结构
CAS号：487021-52-3

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AR-A014418 纯度/质量文件产品仅供科研

货号：A174426 标准纯度： 99%+ 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Cell,2024. Ambeed. [ A125712 ]; • Cancer Discov., 2024. Ambeed. [ A285925 ]; • JMC, 2024, 67(17): 14974-14985. Ambeed. [ A288696 ]; • JMC, 2024, 67(17): 15061-15079. Ambeed. [ A524399 , A633512 , A144280 , A174613 ]; • EJNMMI Radiopharm. Chem., 2024, 9, 61. Ambeed. [ A1257961 , A622068 ]; 更多 >

GSK-3 亚型比较

产品名称	GSK-3 ↓ ↑	GSK-3α ↓ ↑	GSK-3β ↓ ↑	纯度
AZD2858	+ GSK-3, IC50: 68 nM			98+%
Bikinin	✔			99%+
GSK 3 Inhibitor IX	++++ GSK-3, IC50: 5 nM			99%+
AZD1080		+++ GSK-3α, IC50: 6.9 nM	++ GSK-3β, IC50: 31 nM	99%+
BIO-acetoxime		+++ GSK-3α, IC50: 10 nM	+++ GSK-3β, IC50: 10 nM	95%
SB-216763		++ GSK-3α, IC50: 34.3 nM	++ GSK-3β, IC50: ~34.3 nM	98%
SB 415286		+ GSK-3α, IC50: 78 nM	+ GSK-3β, IC50: ~78 nM	99%+
CHIR-98014		++++ GSK-3α, IC50: 0.65 nM	++++ GSK-3β, IC50: 0.58 nM	98%
LY2090314		++++ GSK-3α, IC50: 1.5 nM	++++ GSK-3β, IC50: 0.9 nM	99%+
CHIR 99021		+++ GSK-3α, IC50: 10 nM	++++ GSK-3β, IC50: 6.7 nM	99%+
TDZD-8			+ GSK-3β, IC50: 2 μM	99%+
Indirubin			+ GSK-3β, IC50: 0.6 μM	98%
IM-12			++ GSK-3β, IC50: 53 nM	98%
TWS119			++ GSK-3β, IC50: 30 nM	98%
1-Azakenpaullone			+++ GSK-3β, IC50: 18 nM	99%+
AR-A014418			++ GSK-3β, Ki: 38 nM	99%+
Tideglusib			+ GSK-3β, IC50: 60 nM	98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

AR-A014418 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 (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].

AR-A014418 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

AR-A014418 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.

AR-A014418 实验方案

计算器

存储液制备

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

AR-A014418 技术信息

CAS号	487021-52-3
分子式	C₁₂H₁₂N₄O₄S
分子量	308.313

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

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

AR-A014418 99%+

AR-A014418 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

AR-A014418 质控信息

AR-A014418 生物活性

AR-A014418 细胞研究

AR-A014418 参考文献

AR-A014418 实验方案

AR-A014418 技术信息

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AR-A014418 99%+

AR-A014418 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

AR-A014418 质控信息

AR-A014418 生物活性

AR-A014418 细胞研究

AR-A014418 参考文献

AR-A014418 实验方案

AR-A014418 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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AR-A014418 纯度/质量文件产品仅供科研