MG-132

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Chemical Structure| 133407-82-6 同义名 : Z-Leu-Leu-Leu-al; Z-Leu-Leu-Leu-CHO; MGI-132; (S)-MG132; MG132 SSS
CAS号 : 133407-82-6
货号 : A181909
分子式 : C26H41N3O5
纯度 : 99%+
分子量 : 475.62
MDL号 : MFCD00674886
存储条件：

Pure form Inert atmosphere, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(220.76 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
描述 Proteasome and calpain are the main nonlysosomal proteases responsible for intracellular proteolysis. MG-132 is a potent cell-permeable inhibitor of both proteasome and calpain with respective IC50 values of 0.1µM and 1.25µM. MG-132 induced neurite outgrowth in PC12 cells at a concentration of 20nM. In rabbit erythrocytes, MG-132 penetrated cell membrane and inhibited the autolysis at the dose of 100µM[3]. MG-132 also showed inhibitory activity on cell growth in both human ocular melanoma IPC227F cells and murine melanoma B16 cells with IC50 values of 42 and 77nM, respectively[4]. In airway epithelial cells, pretreatment with 10μM MG-132 for 1h inhibited TNF-α-stimulated IL-8 protein production and release. Moreover, preincubation of cells with 10μM MG-132 reversed the effects of TNF-α on the transcriptional activity of IL-8 gene, IκB degradation, and NF-κB activation[5]. In mice with hindlimb immobilization, twice-daily subcutaneous injections of MG-132 (7.5 mg/kg/dose) significantly increased the running time on treadmill as compared to DMSO-treated group. However, no significant difference in the running time of MG132- and DMSO-treated mice was observed after 11 days of remobilization[6].
作用机制 MG-132 inhibits proteasome primarily via acting on the chymotrypsin-like site in the  subunit. It also inhibits the caspase-like site at high concentrations[7].
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
293T 10 μM Cytotoxic Assay 72 h IC50<2 μM 24625088
293T 10 μM Function Assay 24 h Moderately induces heat-shock 24625088
697 Growth Inhibition Assay IC50=14.4511 μM SANGER
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.10mL

0.42mL

0.21mL

10.51mL

2.10mL

1.05mL

21.03mL

4.21mL

2.10mL
参考文献

[1]Fiedler MA, Wernke-Dollries K, Stark JM. 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. 1998;19(2):259-68.

[2]Tsubuki S, Saito Y, et al. Differential inhibition of calpain and proteasome activities by peptidyl aldehydes of di-leucine and tri-leucine. J Biochem. 1996;119(3):572-6.

[3]Tsubuki S, Saito Y, Tomioka M, Ito H, Kawashima S. Differential inhibition of calpain and proteasome activities by peptidyl aldehydes of di-leucine and tri-leucine. J Biochem. 1996 Mar;119(3):572-6.

[4]Vivier M, Rapp M, Papon J, Labarre P, Galmier MJ, Sauzière J, Madelmont JC. Synthesis, radiosynthesis, and biological evaluation of new proteasome inhibitors in a tumor targeting approach. J Med Chem. 2008 Feb 28;51(4):1043-7.

[5]Fiedler MA, Wernke-Dollries K, Stark JM. 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. 1998 Aug;19(2):259-68.

[6]Caron AZ, Haroun S, Leblanc E, Trensz F, Guindi C, Amrani A, Grenier G. The proteasome inhibitor MG132 reduces immobilization-induced skeletal muscle atrophy in mice. BMC Musculoskelet Disord. 2011 Aug 15;12:185.

[7]Goldberg AL. Development of proteasome inhibitors as research tools and cancer drugs. J Cell Biol. 2012 Nov 12;199(4):583-8.