MG-132  (Synonyms: Z-Leu-Leu-Leu-al)

MG-132 (GMP) (Z-Leu-Leu-Leu-al (GMP)) is MG-132 (HY-13259) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. MG-132 (Z-Leu-Leu-Leu-al) is a potent proteasome and calpain inhibitor with IC₅₀s of 100 nM and 1.2 μM, respectively. MG-132 effectively blocks the proteolytic activity of the 26S proteasome complex. MG-132, a peptide aldehyde, also is an autophagy activator. MG-132 also induces apoptosis^[1][2][3].

MG-132 (GMP) (Z-Leu-Leu-Leu-al) 在低浓度 (30 nM) 下启动 PC12 细胞的神经突生长，是一种非常强的 20S 蛋白酶体抑制剂^[3]。
MG-132 (GMP) (10 μM；1 小时) 可逆转 A549 细胞中 TNF-α 对 IκB 降解和 NF-κ B 活化的影响^[4]。
MG-132 (GMP) (0.75-5 μM；24 小时) 通过 26S 蛋白酶体抑制作用在 KIM-2 细胞中有效诱导 p53 依赖性细胞凋亡^[5]。
MG-132 (GMP) (10-40 μM；24小时) 以时间依赖性和浓度依赖性方式显著降低 C6 神经胶质瘤细胞的活力，并显示 IC₅₀ 在 24 小时时为 18.5 μM^[6]。
MG-132 (GMP) (18.5 μM；24 小时) 诱导抗凋亡蛋白 Bcl-2 和 XIAP 的下调，并上调促凋亡蛋白 Bax 和 caspase-3 的表达^[6]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

MG-132 (GMP) (10 mg/kg；腹腔注射；从注射 EC9706 细胞后 5 天开始每天施用 25 天) 显著抑制 EC9706 异种移植物的肿瘤生长，而不会对小鼠造成毒性^[7]。
MG-132 (GMP) (1 mg/kg；静脉注射；每周两次，持续 4 周) 对携带 HeLa 肿瘤的小鼠显示出有效的肿瘤抑制作用^[8]。
MG-132 (GMP) (1-10 μg/kg/day；皮下植入渗透泵；持续 8 天) 显著增加小鼠骨骼肌裂解液中 β-肌营养不良聚糖、α-肌营养不良聚糖、α-肌肌聚糖和抗肌萎缩蛋白的表达水平 (6 月龄雄性 C57BL/10ScSn DMD mdx 小鼠)^[9]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

475.62

C₂₆H₄₁N₃O₅

133407-82-6

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Harhouri K, et al. MG132-induced progerin clearance is mediated by autophagy activation and splicing regulation. EMBO Mol Med. 2017 Sep;9(9):1294-1313.  [Content Brief]

  [2]. Fan WH, et al. Proteasome inhibitor MG-132 induces C6 glioma cell apoptosis via oxidative stress. Acta Pharmacol Sin. 2011 May;32(5):619-25.  [Content Brief]

  [3]. Tsubuki S, et al. Differential inhibition of calpain and proteasome activities by peptidyl aldehydes of di-leucine and tri-leucine. J Biochem. 1996 Mar;119(3):572-6.  [Content Brief]

  [4]. 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. 1998 Aug;19(2):259-68.  [Content Brief]

  [5]. MacLaren AP, et al. p53-dependent apoptosis induced by proteasome inhibition in mammary epithelial cells. Cell Death Differ. 2001 Mar;8(3):210-8.  [Content Brief]

  [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. 2009 Jul;22(1):215-21.  [Content Brief]

  [7]. Dang L, et al. Proteasome inhibitor MG132 inhibits the proliferation and promotes the cisplatin-inducedapoptosis of human esophageal squamous cell carcinoma cells. Int J Mol Med. 2014 May;33(5):1083-8.  [Content Brief]

  [8]. Matsumoto Y, et al. Enhanced efficacy against cervical carcinomas through polymeric micelles physically incorporating theproteasome inhibitor MG132. Cancer Sci. 2016 Jun;107(6):773-81.  [Content Brief]

  [9]. 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. 2003 Oct;163(4):1663-75.  [Content Brief]