产品信息

产品简介：

MG-132是一种蛋白酶体抑制剂，IC50为100 nM，也抑制钙蛋白酶，IC50为1.2 μM。MG132通过诱导细胞周期停滞以及引发细胞凋亡来抑制HeLa细胞的生长。MG-132 (10 μM) 通过抑制蛋白酶体介导的IκBα降解，有效抑制A549细胞中TNF-α诱导的NF-κB活化。体内研究中，MG-132（ip，0.1 mg/kg/day）通过调节ERK1/2和JNK1信号通路，减轻压力超负荷引起的心脏肥大。MG-132治疗通过下调肌肉特异性泛素连接酶atrogin-1/MAFbx 和MuRF-1 mRNA，显著减少小鼠体内固定化诱导的骨骼肌萎缩。

本品以冻干粉形式提供，纯度≥98%，可溶于DMSO或无水乙醇配制成储存液，之后用培养基或生理缓冲液稀释到需要的工作浓度即可。

产品性质

英文别名（English Synonym）： MG132; MG 132; Z-Leu-Leu-Leu-CHO; Z-Leu-Leu-Leu-al; Z-LLL-CHO;Carbobenzoxy-L-leucyl- L-leucyl-L-leucinal

化学名（Chemical Name）：N-[(phenylmethoxy)carbonyl]-L-leucyl-N-[(1S)-1-formyl-3-methylbutyl]-L-leucinamide

靶点（Target）：ChTL(20S Proteasomes)/ 0.22 μM, PGPH(20S Proteasomes)/2.95 μM，TL(20S Proteasomes)/34.4 μM

CAS 号（CAS NO.）：133407-82-6

分子式（Molecular Formula）：C26H41N3O5

分子量（Molecular Weight）：475.6

外观（Appearance）：白色至类白色固体

纯度（Purity）：＞98%

溶解性（Solubility）：溶于DMSO（30 mg/ml），无水乙醇（20mg/ml）

运输与保存方法

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

相关产品：

使用浓度

【具体使用浓度请参考相关文献，并根据自身实验条件（如实验目的，细胞种类，培养特性等）进行摸索和优化。】

1） 使用前置于室温回温至少20min，并经短暂离心使得粉末/固体落在管底后再溶解。

2） 称取适量粉末溶于无水DMSO配制储存液（比如20 mg/ml，取500μl DMSO 加入10mg MG-132，涡旋混匀，直至完全溶解）。按照单次用量分装后-20ºC保存，避免反复冻存，至少1个月稳定， 也可置于-80℃延长保存周期。

3） 根据具体实验应用，选择合适的溶剂稀释到所需浓度。体外细胞实验，常用的工作浓度是5-50 µM，处理时间1-24h。本品的具体工作浓度和处理时间请参考相关文献，并根据自身实验条件（如实验目的，细胞种类，培养特性等）进行摸索和优化。

相关实验（数据来自于公开发表的文献，仅供参考）

使用方法【源自文献，仅作参考】

文献1，MacLaren AP et al. p53-dependent apoptosis induced by proteasome inhibition in mammary epithelial cells. Cell Death Differ. 2001 Mar;8(3):210-8. PMID: 11319603

体外研究：

细胞类型（Cell type）：HeLa cells exposed to 10 or 100 J/m2 UV (254 nm) using a UV crosslinker.

药物配制（Preparation）：MG132 dissolved in DMSO and diluted in DMEM.

实验方法（Assay）：HeLa cells were grown to about 60% confluence in DMEM at 37°C in the presence of 5% CO2. MG132 dissolved in DMSO was added (5 µM final concentration). For mock treatment, DMSO alone was added. Cells were incubated for 1 h before UV irradiation. For UV treatment, medium in the Petri dishes was removed, and cells were exposed to 10 or 100 J/m2 UV (254 nm) using a UV crosslinker. Medium containing MG132 or DMSO alone was added back to the respective Petri dishes, and cells were transferred back to the incubator for the time course experiment.

文献2，Inoue S et al.The effect of proteasome inhibitor MG132 on experimental inflammatory bowel disease. Clin Exp Immunol. 2009 Apr;156(1):172-82. PMID: 19220323

体内研究：

动物模型（Animal Model）：Experimental murine colitis models: IL-10-deficient (IL-10−/−) mice and dextran sulphate sodium (DSS)-induced colitis

药物配制（Preparation）：MG132 was dissolved in dimethyl sulphoxide (DMSO) and then diluted in 500 µl sterile phosphate-buffered saline (PBS) for injection.

注射剂量（Dosages）：Female IL-10−/− mice at 4 weeks of age were divided into four groups and treated with intraperitoneal injection three times a week as follows: group A, 0·01% DMSO as the control; group B, 0·6 µmol/kg MG132; group C, 3·0 µmol/kg MG132; and group D, 15·0 µmol/kg MG132. All mice were killed after 4 weeks of treatment by cervical dislocation under ether anaesthesia.

Female C57BL/6 mice were given 3% DSS (molecular weight 36–50 kDa) in their drinking water for 5 days, and then switched to regular drinking water. Mice were injected intraperitoneally with 15·0 µmol/kg MG132 (prepared in the same way as for IL-10−/− mice) or 0·01% DMSO as the control three times a week from day 0 to the end of the experiment. On day 10, the mice were killed.

给药途径（Administration）：Intraperitoneal (i.p.) injection

参考文献

1. 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.

2. 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.

3. 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.

4. 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.

5. Caron AZ, et al. The proteasome inhibitor MG132 reduces immobilization-induced skeletal muscle atrophy in mice. BMC Musculoskelet Disord. 2011 Aug 15;12:185.