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SB 415286,GSK-3 抑制劑,GSK-3 inhibitors
  • SB 415286,GSK-3 抑制劑,GSK-3 inhibitors
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貨物所在地:上海上海市

地: 德國

更新時間:2024-08-28 21:00:26

瀏覽次數:50

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SB 415286,GSK-3 抑制劑,GSK-3 inhibitors
分子量 (MW):359.72
化學式:C16H10ClN3O5
溶解度: DMSO 72mg/mL Water <1mg/mL Ethanol 72mg/mL
穩定性:at -20℃ 2 years
CAS號:264218-23-7

上海義森生物科技有限公司提供:SB 415286,GSK-3 抑制劑,GSK-3 inhibitors

 

生物活性

技術數據:

分子量(MW): 359.72 SB 415286 Chemical Structure
化學式:

C16H10ClN3O5

溶解度: DMSO 72mg/mL   Water <1mg/mL   Ethanol 72mg/mL
純度: >99%
穩定性: at -20℃ 2 years
CAS號: 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]

 

參考文獻

  • 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
上海義森生物科技有限公司提供:SB 415286,GSK-3 抑制劑,GSK-3 inhibitors

 

 

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