SB 415286 | Apoptosis Inducer | AmBeed-信号通路专用抑制剂

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SB 415286 99%+

货号：A984794

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

SB 415286 化学结构
CAS号：264218-23-7

SB 415286 3D分子结构
CAS号：264218-23-7

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SB 415286 纯度/质量文件产品仅供科研

货号：A984794 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。

SB 415286 生物活性

靶点

GSK-3α

GSK-3α, IC50:78 nM
GSK-3β

GSK-3β, IC50:~78 nM

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].

SB 415286 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
CHO cells		Function assay		Stimulation of glycogen synthase in CHO cells expressing human insulin receptor, EC50=45.6 μM	12852764

SB 415286 参考文献

[1]Cross DA, Culbert AA, et al. Selective small-molecule inhibitors of glycogen synthase kinase-3 activity protect primary neurones from death. J Neurochem. 2001 Apr;77(1):94-102.

[2]Coghlan MP, Culbert AA, et al. Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription. Chem Biol. 2000 Oct;7(10):793-803.

[3]Coghlan MP, Culbert AA, et al. Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription. Chem Biol. 2000 Oct;7(10):793-803

[4]Dickey A, Schleicher S, Leahy K, Hu R, Hallahan D, Thotala DK. GSK-3β inhibition promotes cell death, apoptosis, and in vivo tumor growth delay in neuroblastoma Neuro-2A cell line. J Neurooncol. 2011 Aug;104(1):145-53

SB 415286 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.78mL

0.56mL

0.28mL

13.90mL

2.78mL

1.39mL

27.80mL

5.56mL

2.78mL

SB 415286 技术信息

CAS号	264218-23-7
分子式	C₁₆H₁₀ClN₃O₅
分子量	359.721

别名
运输	蓝冰

存储条件

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 105 mg/mL(291.89 mM)，配合低频超声助溶，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

SB 415286 99%+

SB 415286 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

SB 415286 质控信息

SB 415286 生物活性

SB 415286 细胞研究

SB 415286 参考文献

SB 415286 实验方案

SB 415286 技术信息

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SB 415286 99%+

SB 415286 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

SB 415286 质控信息

SB 415286 生物活性

SB 415286 细胞研究

SB 415286 参考文献

SB 415286 实验方案

SB 415286 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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SB 415286 纯度/质量文件产品仅供科研