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MG-132

Catalog No.
A2585
细胞通透性的、可逆性的蛋白酶体抑制剂。
组合的产品项目
规格价格库存 数量
10mg
¥ 500.00
现货
25mg
¥ 1,200.00
现货
50mg
¥ 2,200.00
现货
100mg
¥ 3,200.00
现货
500mg
¥ 9,800.00
现货

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Background

MG132 (carbobenzoxy-Leu-Leu-leucinal) as a peptide aldehyde effectively blocks the proteolytic activity of proteasome complex.9 Proteasome inhibitors including MG132 have been shown to induce apoptotic cell death through formation of ROS. ROS formation and GSH depletion due to proteasome inhibitors may cause mitochondrial dysfunction and subsequent cytochrome c release, which leads to cell viability loss1, 2.

MG132 dose dependently inhibited the growth of A549 cells with an IC50 of approximately 20 µM. MG132 also reduced the growth of human cervical HeLa cancer cells with an IC50 of approximately 5 µM. Treatment with 0.5 µM MG132 significantly decreased the growth of HeLa cells and induced cell death as well. Cell growth inhibition by MG132 depends on incubation doses of that and cell types3.

MG132 significantly induced a G1 phase arrest of the cell cycle. It inhibits the growth of HT-29 colon cancer cells via inducing G2/M cell cycle arrest4, causes MG-63 osteosarcoma cell arrest at G2/M phase5, prolongs the duration of G0/G1 arrest in MnCl2-treated A549 cells21 and induces a G1 arrest in gastric carcinoma cells6. Deregulation of the ubiquitin-proteasomal system by MG132 can result in different cell cycle phase arrests depending on various cancer cell lines.

Proteasome inhibitors including MG132 have been shown to induce apoptotic cell death through formation of ROS1, 2, 7.  MG132 inhibited the growth of human A549 cells via inducing the cell cycle arrest as well as triggering apoptosis, which was in part correlated with the changes of ROS and GSH levels.

References:
1. Ling YH, Liebes L, Zou Y and Perez-Soler R. Reactive oxygen species generation and mitochondrial dysfunction in the apoptotic response to Bortezomib, a novel proteasome inhibitor, in human H460 non-small cell lung cancer cells, 2003; 278: 33714–33723.
2. Qiu JH, Asai A, Chi S, et al. Proteasome inhibitors induce cytochrome c-caspase-3-like protease-mediated apoptosis in cultured cortical neurons. J Neurosci 2000; 20: 259–265.
3. YH. Han, WH. Park, MG132 as a proteasome inhibitor induces cell growth inhibition and cell death in A549 lung cancer cells via influencing reactive oxygen species and GSH level, Human and Experimental Toxicology, 29(7) 607–614.
4. Wu WK, Wu YC, Yu L, et al. Induction of autophagy by proteasome inhibitor is associated with proliferative arrest in colon cancer cells. Biochem Biophys Res Commun 2008; 374: 258–263.
5. Yan XB, Yang DS, Gao X, et al. Caspase-8 dependent osteosarcoma cell apoptosis induced by proteasome inhibitor MG132. Cell Biol Int 2007; 31: 1136–1143.
6. ZhangW, Tong Q, Li S, Wang X andWang Q.MG-132 inhibits telomerase activity, induces apoptosis and G(1) arrest associated with upregulated p27kip1 expression and downregulated survivin expression in gastric carcinoma cells. Cancer Invest 2008; 26:1032–1036.
7. Wu HM, Chi KH, Lin WW. Proteasome inhibitors stimulate activator protein-1 pathway via reactive oxygen species production. FEBS Lett 2002; 526: 101–105.

文献引用

Chemical Properties

StorageStore at -20°C
该产品在溶液中不稳定,建议现配现用
M.Wt475.6
Cas No.133407-82-6
FormulaC26H41N3O5
SynonymsMG132,Z-LLL-al,Z-Leu-Leu-Leu-CHO
Solubility≥23.78mg/mL in DMSO
Chemical Namebenzyl N-[(2S)-4-methyl-1-[[(2S)-4-methyl-1-[[(2S)-4-methyl-1-oxopentan-2-yl]amino]-1-oxopentan-2-yl]amino]-1-oxopentan-2-yl]carbamate
SDFDownload SDF
Canonical SMILESCC(C)CC(C=O)NC(=O)C(CC(C)C)NC(=O)C(CC(C)C)NC(=O)OCC1=CC=CC=C1
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

激酶实验:

MG-132对蛋白酶体9的抑制活性

MG-132是一种肽醛,可以有效阻断蛋白酶体9的蛋白水解活性。已有研究表明,蛋白酶体的抑制剂 (包括MG-132)通过形成活性氧(ROS)从而诱导凋亡性细胞死亡。蛋白酶体抑制剂引起的ROS的形成和谷胱甘肽(GSH)的耗竭可能导致线粒体功能障碍和随后细胞色素c的释放,从而导致细胞活力的丧失[1,2]。

细胞实验:

细胞系

A549细胞、人宫颈癌HeLa细胞、HT-29结肠癌细胞、MG-63骨肉瘤细胞等。

溶解方法

在DMSO中的溶解度>23.8mg/mL。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应时间

24-48小时

应用

MG-132是一种膜通透性的蛋白酶体抑制剂。在PC12细胞中,MG-132(10 μM) 可用于诱导神经突触的生长。MG-132剂量依赖地抑制A549细胞的生长,IC50值为20 μM。MG-132也可以抑制人宫颈癌Hela细胞的生长,IC50值约为5 μM。0.5 μM的MG-132就可以显著减少Hela细胞的生长,诱导细胞死亡[3]。MG-132通过诱导G2 / M期细胞周期停滞从而抑制HT-29结肠癌细胞和MG-63骨肉瘤细胞的生长[5]。在氯化锰处理的A549细胞中,MG-132延长G0 / G1期停滞的时间。MG-132也可以诱导胃癌细胞中G1期停滞[6]。

动物实验:

动物模型

C57BL小鼠

剂量

~10 μg/kg/天,尾静脉或腹腔注射。

溶解方法

溶解于DMSO中用于制备10 mg/ml的储备原液,工作液可用PBS或生理盐水进行稀释,pH等于7。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

References:

1. Ling YH, Liebes L, Zou Y and Perez-Soler R. Reactive oxygen species generation and mitochondrial dysfunction in the apoptotic response to Bortezomib, a novel proteasome inhibitor, in human H460 non-small cell lung cancer cells, 2003; 278: 33714–33723.

2. Qiu JH, Asai A, Chi S, et al. Proteasome inhibitors induce cytochrome c-caspase-3-like protease-mediated apoptosis in cultured cortical neurons. J Neurosci 2000; 20: 259–265.

3. YH. Han, WH. Park, MG132 as a proteasome inhibitor induces cell growth inhibition and cell death in A549 lung cancer cells via influencing reactive oxygen species and GSH level, Human and Experimental Toxicology, 29(7) 607–614.

4. Wu WK, Wu YC, Yu L, et al. Induction of autophagy by proteasome inhibitor is associated with proliferative arrest in colon cancer cells. Biochem Biophys Res Commun 2008; 374: 258–263.

5. Yan XB, Yang DS, Gao X, et al. Caspase-8 dependent osteosarcoma cell apoptosis induced by proteasome inhibitor MG132. Cell Biol Int 2007; 31: 1136–1143.

6. ZhangW, Tong Q, Li S, Wang X andWang Q.MG-132 inhibits telomerase activity, induces apoptosis and G(1) arrest associated with upregulated p27kip1 expression and downregulated survivin expression in gastric carcinoma cells. Cancer Invest 2008; 26:1032–1036.

生物活性

描述 MG-132是一种蛋白酶体抑制剂,IC50为100 nM,也可以抑制钙蛋白酶,IC50为1.2 μM。
靶点 Proteasome          
IC50 100 nM          

质量控制

质量控制和MSDS

批次:

相关生物数据

MG-132

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