分子生物学
IVD分子诊断
细胞培养与分析
蛋白研究
细胞因子
重组蛋白
抗体
高通量测序建库
病原检测UCF系列
生物医药
工具酶
抑制剂激活剂与常用试剂
仪器
耗材
MG132 (MG-132)
99元起解锁高分小分子化合物,5月1-31日
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MG132 (MG-132, Z-Leu-Leu-Leu-al, Z-Leu-Leu-Leu-CHO)是强效的、可逆的、细胞通透性proteasome抑制剂(IC50 = 100 nM),抑制20S蛋白酶体的ZLLL-MCA降解活性时,比ZLLal有效1000多倍。MG132也可以抑制细胞周期和细胞周期蛋白降解所需要的calpain (IC50 = 1.2 μM),并诱导PC12细胞中神经突增生。另外,MG132抑制IκBα降解,从而抑制NF-κB通路活化。MG132诱导MPM细胞凋亡,并伴随caspase 3、7、8、9蛋白活化。MG132还诱导线粒体膜电位变化,而且细胞内ROS水平也会提高。

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参考文献

[1] Tsubuki S, et al. Differential inhibition of ca pain and proteasome activities by peptidyl aldehydes of di-leucine and tri-leucine. J Biochem, 119(3): 572-576 (1996).

[2] Fiedler MA, et al. Inhibition of TNF-alpha-induced NF-kappaB activation and IL-8 release in A549 cells with the proteasome inhibitor MG-132. Am J Respir Cell Mol Biol, 19(2): 259-268 (1998).

[3] Bonuccelli G, et al. Proteasome inhibitor (MG-132) treatment of mdx mice rescues the expression and membrane localization of dystrophin and dystrophin-associated proteins. Am J Pathol, 163(4): 1663-1675 (2003).

[4] Bao-Zhu Yuan, et al. Proteasome Inhibitor MG132 Induces Apoptosis and Inhibits Invasion of Human Malignant Pleural Mesothelioma Cells. Transl Oncol. 1(3): 129–140 (2008).

[5] Steinhilb ML, et al. The Protease Inhibitor, MG132, Blocks Maturation of the Amyloid Precursor Protein Swedish Mutant Preventing Cleavage by β-Secretase. J. Biol.Chem, 276: 4476 (2001).

[6] Han YH, et al. The effect of MG132, a proteasome inhibitor on HeLa cells in relation to cell growth, reactive oxygen species and GSH. Oncol Rep. 22(1): 215-21(2009).

存储条件

粉末直接保存于-20 ºC,有效期2年。溶于DMSO,建议分装后-20ºC避光保存,避免反复冻存,至少可存放6个月。

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