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MG-132

MG-132 (Z-Leu-Leu-Leu-al) 是一种 26S 蛋白酶体抑制剂 (IC50=100 nM)，具有细胞渗透性、可逆性。MG-132 可作为自噬激活剂，可诱导凋亡。

CAS号

133407-82-6

分子式

C26H41N3O5

主要靶点

Proteasome|Apoptosis|Autophagy

仅限科研使用

Cat No : CM00367

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Synonyms

complex|20S proteasome|26S|calpain|Autophagy|Apoptosis|aldehyde|inhibit|Inhibitor|MG 132|MG132|MG-132|Proteasome|proteolytic|Z-LLL-al|Z-Leu-Leu-Leu-CHO|peptide

验证数据展示

  • CAS No.: 133407-82-6

    MG-132
    CAS#: 133407-82-6

产品信息

MG-132 (Z-Leu-Leu-Leu-al) is a 26S proteasome inhibitor (IC50=100 nM) that is cell-permeable and reversible. MG-132 acts as an autophagy activator and also induces apoptosis.

CAS号 133407-82-6
分子式 C26H41N3O5
主要靶点 Proteasome|Apoptosis|Autophagy
主要通路 泛素化|蛋白酶体|凋亡|自噬
分子量 475.62
纯度 99.69%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
别名 complex|20S proteasome|26S|calpain|Autophagy|Apoptosis|aldehyde|inhibit|Inhibitor|MG 132|MG132|MG-132|Proteasome|proteolytic|Z-LLL-al|Z-Leu-Leu-Leu-CHO|peptide

靶点活性

HCT116 cells:0.82 μM|20S proteasome:100 nM (cell free)|Calpain:1.2 μM (cell free)|COS-7 cells:< 10 μM

体内活性

方法：为检测体内抗肿瘤活性，将 MG-132 (1 mg/kg) 静脉注射给携带人宫颈癌肿瘤 HeLa、CaSki 或 C33A 的 C.B‐17/lcr‐scid/scidJcl 小鼠，每周两次，持续四周。_x000D_ 结果：MG-132 治疗显著抑制人宫颈癌肿瘤的生长，表明在体内具有抗肿瘤活性。[4]_x000D_ 方法：为研究 MG-132 长期治疗对心肌肥大的影响及其相关分子机制，将 MG-132 (0.1 mg/kg) 腹腔注射给具有腹主动脉束带（AAB）的大鼠，每天一次，持续八周。_x000D_ 结果：MG-132 治疗显著减弱了 AAB 大鼠的左心室肌细胞面积、左心室重量/体重和肺重量/体重比，降低了左心室舒张直径和壁厚，并增加了缩短分数。MG-132 治疗可显著逆转 AAB 大鼠 ERK1/2 和 JNK1 磷酸化水平的升高。[5]

体外活性

方法：人宫颈癌细胞 HeLa 用 MG-132 (0.5-30 μM) 处理 24 h，使用 MTT 方法检测细胞生长抑制情况。_x000D_ 结果：MG-132 剂量依赖性地抑制 HeLa 细胞生长，IC50 约为 5 μM。[1]_x000D_ 方法：人间皮瘤细胞 NCI-H2452 用 MG-132 (0.25-2 μM) 处理 36 h，使用 Western Blot 方法检测靶点蛋白表达水平。_x000D_ 结果：MG-132 处理诱导 NCI-H2052 细胞中 caspases 3、caspases 7、Bid 和 PARP 的切割，诱导 caspase 依赖性凋亡。[2]_x000D_ 方法：人类黑色素瘤细胞 MeWo 用 MG-132 (0.01-1 μM) 处理 24 h，使用 Flow Cytometry 方法分析细胞周期情况。_x000D_ 结果：MG-132 诱导 MeWo 细胞的细胞周期阻滞在 G2 期。[3]

溶解度

10% DMSO+40% PEG300+5% Tween 80+45% Saline:9 mg/mL (18.92 mM);DMSO:240 mg/mL (504.6 mM);Ethanol:47.5 mg/mL (99.87 mM);H2O:Insoluble

参考文献

1.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.
2.Yuan BZ, et al. Proteasome Inhibitor MG132 Induces Apoptosis and Inhibits Invasion of Human Malignant Pleural Mesothelioma Cells. Transl Oncol. 2008 Sep;1(3):129-40.
3.Braun HA, et al. Tripeptide mimetics inhibit the 20 S proteasome by covalent bonding to the active threonines. J Biol Chem. 2005 Aug 5;280(31):28394-401.
4.Matsumoto Y, et al. Enhanced efficacy against cervical carcinomas through polymeric micelles physically incorporating the proteasome inhibitor MG132.  Cancer Sci. 2016 Jun;107(6):773-81.
5.Chen B, et al. MG132, a proteasome inhibitor, attenuates pressure-overload-induced cardiac hypertrophy in rats by modulation of mitogen-activated protein kinase signals. Acta Biochim Biophys Sin (Shanghai). 2010 Apr;42(4):253-8.
6.Caron AZ, et al. The proteasome inhibitor MG132 reduces immobilization-induced skeletal muscle atrophy in mice. BMC Musculoskelet Disord. 2011 Aug 15;12:185.
7.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.
8.Guzmán-Téllez P, Martínez-Valencia D, Silva-Olivares A, et al. Naegleria fowleri and Naegleria gruberi 20S proteasome: identification and characterization[J]. European Journal of Cell Biology. 2020: 151085

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