SB 415286

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Chemical Structure| 264218-23-7 同义名 : -
CAS号 : 264218-23-7
货号 : A984794
分子式 : C16H10ClN3O5
纯度 : 99%+
分子量 : 359.721
MDL号 : MFCD04039789
存储条件：

Pure form Inert atmosphere,Store in freezer, under -20°C

In solvent -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：
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 Ki 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
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
实验方案
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
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