MG-132（Z-Leu-Leu-Leu-CHO）；Proteasome Inhibitor蛋白酶体抑制剂；Calpain Inhibitor钙蛋白酶抑制剂；；NF-κB activation；CAS：133407-82-6；
MG-132（MG132，MG 132），也称为Z-Leu-Leu-Leu-al，Z-Leu-Leu-Leu-CHO，是一种强效的，可逆且具细胞渗透性的蛋白酶体Proteasome抑制剂（IC50=100 nM），还是细胞周期和细胞周期蛋白降解所需的钙蛋白酶Calpain抑制剂（IC50=1.2 μM）[1]。A549细胞中MG-132（10μM）有效抑制TNFα诱导的NF-κB活化、IL-8基因转录和IL-8蛋白分泌，通过抑制蛋白酶体介导的IκBα降解来发挥作用[2]。MG-132（10μM）对NF-κB的抑制效应促使人胰腺癌细胞对依托泊甙Etoposide或阿霉素Doxorubicin的凋亡诱导更加敏感[3]。在PC3和DU145雄激素非依赖的前列腺癌（AIPCa）细胞系中MG-132能显著改善六磷酸肌醇（IP6）对细胞代谢的减低能力[4]。
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。
产品特性
1）CAS NO：133407-82-6
2）化学名：N-[(phenylmethoxy)carbonyl]-L-leucyl-N-[(1S)-1-formyl-3-methylbutyl]-L-leucinamide
3）同义名：MG132; MG 132; Z-Leu-Leu-Leu-CHO; Z-Leu-Leu-Leu-al; Z-LLL-CHO;Carbobenzoxy-L-leucyl- L-leucyl-L-leucinal;
4）分子式：C26H41N3O5
5）分子量：475.6
6）纯度：≥98%
7） 外观：白色至类白色固体
8）溶解性：溶于DMSO（30 mg/ml），无水乙醇（20mg/ml）
保存与运输方法
保存：-20℃干燥保存，至少2年有效。
运输：常温运输。
产品使用
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。
文献使用数据【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 |
注意事项
1）本品仅用作科研用途，不得用作临床诊断或治疗，不得用于食品或药品，绝对禁止用在人身上。
2）为了您的安全和健康，请穿实验服并戴一次性手套操作。
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,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] A. Arlt, J. Vorndamm, M. Breitenbroich, et al. Inhibition of NF- k B sensitizes human pancreatic carcinoma cells to apoptosis induced by etoposide (VP16) or doxorubicin. Oncogene 20, 859-868 (2001).
[4] Diallo JS, et al. Enhanced killing of androgen-independent prostate cancer cells using inositol hexakisphosphate in combination with proteasome inhibitors. Br J Cancer, 99(10), 1613-1622 (2008).
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