SB 415286 (SB415286, SB-415286)是一种强效的、细胞渗透性的糖原合酶激酶-3 (GSK-3α) 抑制剂,其IC50值为77.5 nM,Ki值为30.75 nM,也可抑制GSK-3β,抑制效果和GSK-3α相同,是GSK-3有效选择性抑制剂。研究表明,SB 415286在人肝细胞中可促进合成糖原,在小鼠中枢神经中起保护作用并修复受损神经元。在原代神经元中,SB 415286可以阻止PI3K途径诱导的细胞死亡。SB 415286抑制GSK3β的活性,抑制雷帕霉素(rapamycin)介导的细胞周期蛋白D1下调和细胞周期停滞。同时,SB 415286损伤p53依赖性的p21和Puma的转录激活,促使p53介导的损伤应答从细胞周期停滞转变为细胞凋亡。
参考文献
[1]. Mirlashari MR, et al. Glycogen synthase kinase-3 (GSK-3) inhibition induces apoptosis in leukemic cells through mitochondria-dependent pathway. Leuk Res. 2012 Apr;36(4):499-508.
[2]. Whittle BJ, et al. Reduction of experimental colitis in the rat by inhibitors of glycogen synthase kinase-3beta. Br J Pharmacol. 2006 Mar;147(5):575-82.
[3]. Dickey A, Schleicher S, et al. 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.
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