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CAS No.: 264218-23-7

SB 415286 Catalog No. CSN16568

Synonyms: SB-415286

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

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生物活性

实验方案

技术信息

生物活性

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].
细胞研究
Cell Data
Cell Lines Concentration Assay Type Time Activity Description Data Sources
CHO cells - Function assay - Stimulation of glycogen synthase in CHO cells expressing human insulin receptor, EC50=45.6 μM 12852764
参考文献

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
CHO cells	-	Function assay	-	Stimulation of glycogen synthase in CHO cells expressing human insulin receptor, EC50=45.6 μM	12852764

[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

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
- 2.7799 mL
- 13.8997 mL
- 27.7993 mL
- 5 mM
- 0.5560 mL
- 2.7799 mL
- 5.5599 mL
- 10 mM
- 0.2780 mL
- 1.3900 mL
- 2.7799 mL

技术信息

CAS号

264218-23-7

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C16H10ClN3O5

运输

蓝冰

分子量

359.72

别名

SB-415286

溶解度

DMSO	83.0 mg/mL (230.7 mM)
Water	insoluble

动物实验配方

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SB 415286 Catalog No. CSN16568

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