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MG-132 目录号 GC10383

Proteasome inhibitor, Cell permeable, reversible

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥473.00
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10mg
¥368.00
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25mg
¥945.00
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100mg
¥2,478.00
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500mg
¥6,731.00
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Sample solution is provided at 25 µL, 10mM.

质量管理

Quality Control & SDS

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实验参考方法

Kinase experiment:

Inhibitory activities of MG-132 towards proteasome complex 9

MG-132 acts as a peptide aldehyde effectively blocks the proteolytic activity of proteasome complex 9. Proteasome inhibitors including MG-132 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 loss [ 1, 2].

Cell experiment:

Cell lines

A549 cells, human cervical HeLa cancer cells, HT-29 colon cancer cells, MG-63 osteosarcoma cell etc.

Preparation method

The solubility of this compound in DMSO is >23.8mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

24-48 h

Applications

MG-132 is a membrane-permeable proteasome inhibitor. It is used to Induce neurite outgrowth in PC12 cells at 10 μM. MG132 dose dependently inhibited the growth of A549 cells with an IC50 of approximately 20 µM. MG-132 also reduced the growth of human cervical HeLa cancer cells with an IC50 of approximately 5 µM. Treatment with 0.5 µM MG-132 significantly decreased the growth of HeLa cells and induced cell death as well [3]. MG-132 inhibits the growth of HT-29 colon cancer cells via inducing G2/M cell cycle arrest [4], causes MG-63 osteosarcoma cell arrest at G2/M phase [5], prolongs the duration of G0/G1 arrest in MnCl2-treated A549 cells and induces a G1 arrest in gastric carcinoma cells [6]. 

Animal experiment [3]:

Animal models

C57BL mice

Dosage form

~10 ug/kg/day, injection from tail vein or belly

Preparation method

Powder dissolved in DMSO to prepare stock solution with 10 mg/ml, and working solution is diluted by PBS or Saline. pH equals to 7.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

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.

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化学数据

Cas No. 133407-82-6 SDF
别名 MG132,Z-LLL-al,Z-Leu-Leu-Leu-CHO
化学名 benzyl 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
Canonical SMILES CC(C)CC(C=O)NC(=O)C(CC(C)C)NC(=O)C(CC(C)C)NC(=O)OCC1=CC=CC=C1
分子式 C26H41N3O5 分子量 475.6
溶解度 ≥23.78mg/mL in DMSO 储存条件 Store at -20°C
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。溶液形式可以在-20℃下储存几个月。
运输条件 所有可选规格:常温运输或根据产品储存温度要求用蓝冰运输。

产品描述

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.