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SB 415286,GSK-3 抑制剂,GSK-3 inhibitors

简要描述:

SB 415286,GSK-3 抑制剂,GSK-3 inhibitors
分子量 (MW):359.72
化学式:C16H10ClN3O5
溶解度: DMSO 72mg/mL Water <1mg/mL Ethanol 72mg/mL
稳定性:at -20℃ 2 years
CAS号:264218-23-7

更新时间:2016-04-03

上海义森生物科技有限公司提供:SB 415286,GSK-3 抑制剂,GSK-3 inhibitors

 

生物活性

技术数据:

分子量(MW): 359.72 SB 415286 Chemical Structure
化学式:

C16H10ClN3O5

溶解度: DMSO 72mg/mL   Water <1mg/mL   Ethanol 72mg/mL
纯度: >99%
稳定性: at -20℃ 2 years
CAS号: 264218-23-7

生物活性

 

SB 415286 is a potent and selective cell-permeable, ATP-competitive GSK3α inhibitor with an IC50 and a Ki of 78 and 31 nM, respectively. SB 415286 competes with ATP. SB 415286 has minimal activity against 24 other protein kinases (IC50 > 10 μ M). SB 415286 stimulates glycogen synthesis, gene transcription and is neuroprotective. As a result of GSK3 inhibition, SB 415286 stimulates glycogen synthesis in the Chang human liver cell line with an EC50 value of 2.9 µM. SB 415286 also protects primary neurons from death induced by the PI3-kinase pathway. In L6 myotubes, SB 415286 induced a much greater activation of GS (6.8-fold) . In adipocytes, SB 415286 caused a comparable activation of GS despite a substantial differentiation-linked reduction in GSK3 expression ( approximay 85%) indicating that GSK3 remains an important determinant of GS activation in fat cells. [1] SB 415286 induced expression of a beta-catenin-LEF/TCF regulated reporter gene in HEK293 cells. [2]

 

参考文献

  • Use of lithium and SB-415286 to explore the role of glycogen synthase kinase-3 in the regulation of glucose transport and glycogen synthase. MacAulay K et al. Eur J Biochem 2003 Sep;270(18):3829-38
  • Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription. Coghlan MP et al. Chem Biol 2000 Oct;7(10):793-803
上海义森生物科技有限公司提供:SB 415286,GSK-3 抑制剂,GSK-3 inhibitors

 

 

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