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。

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).

客户使用本产品发表的科研文献（部分）

[1] Han J, et al. IGF2BP2 Induces U251 Glioblastoma Cell Chemoresistance by Inhibiting FOXO1-Mediated PID1 Expression Through Stabilizing lncRNA DANCR. Front Cell Dev Biol. 2022;9:659228. IF:6.684

[2] Wang SW, et al. Hesperetin promotes DOT1L degradation and reduces histone H3K79 methylation to inhibit gastric cancer metastasis. Phytomedicine. 2021;84:153499. IF:5.340

[3] Tang Z, et al. LncRNA DANCR involved osteolysis after total hip arthroplasty by regulating FOXO1 expression to inhibit osteoblast differentiation. J Biomed Sci. 2018;25(1):4. IF:3.466

[4] Huang J, et al. Functional analysis of a de novo mutation c.1692 del A of the PHEX gene in a Chinese family with X-linked hypophosphataemic rickets. Bone Joint Res. 2019 Sep 3;8(8):405-413. IF: 3.6520

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。