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经验配方 CAS号 C₁₉H₁₂Cl₂N₂O₂ 280744-09-4 描述 概述 A cell-permeable (aryl,indole) maleimide compound that acts as a potent, selective, ATP-competitive inhibitor of GSK-3 activity (Ki = 9.1 nM for GSK-3α). At 10 µM concentration, does not significantly inhibit a panel of 24 other protein kinases tested. Reported to stimulate glycogen synthesis in Chang human liver cells (EC50 = 3.6 µM) and induce transcription of β-catenin-LEF/TCF (lymphoid enhancer factor/T cell factor) regulated reporter gene in HEK293 human embryonic kidney cell lines. Offers protection against polyglutamine-induced death in SK-N-SH and COS-7 cells and attenuates hypoxia-induced apoptosis in VSMC and COS-7 cells. Shown to reduce phosphoenolpyruvate carboxykinase (PEPCK) and glucose-6-phosphatase (G6Pase) expression in hepatoma cells. Promotes the survival of CLL lymphocytes via Wnt/β-catenin-mediated transcription activation. Exhibits delayed cardioprotection in vivo in a rat model via a KATP (ATP-sensitive potassium channels) and MPTP (mitochondrial permeability transition pore)-dependent mechanism at reperfusion. 产品目录编号 361566 品牌系列 Calbiochem®
同义词 SB-216763 参考 参考 Gross, E., et al. 2008. Am. J. Phy. Heart Circ Physiol. 294, H1497.
Bain, J., et al. 2007. Biochem. J. 408, 297.
Lu, D., et al. 2004. PNAS. 101, 3118.
Carmichael, J., et al. 2002. J. Biol. Chem. 277, 33791.
Culbert, A.A., et al. 2001. FEBS Lett. 507, 288.
Lochhead, P.A., et al. 2001. Diabetes 50, 937.
Cross, D.A., et al. 2001. J. Neurochem. 77, 94.
Coghlan, M.P., et al. 2000. Chem. Biol. 7, 793.产品信息 CAS号 280744-09-4 形式 Orange solid Hill配方 C₁₉H₁₂Cl₂N₂O₂ 化学配方 C₁₉H₁₂Cl₂N₂O₂ Molar Mass 371.2 结构配方图像 生物信息 纯度 ≥98% by HPLC 理化信息 溶解度 DMSO 安全信息 R相 R: 36/37/38
Irritating to eyes, respiratory system and skin.S相 S: 26-36
In case of contact with eyes, rinse immediately with plenty of water and seek medical advice.
Wear suitable protective clothing.储存和货运信息 货运代码 Ambient Temperature Only
毒性 Irritant
储存 +2°C to +8°C
无需冷冻 No
特殊指南 Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
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