MG132

MG132 is a potent cell-permeable inhibitor of proteasome and calpain with IC50 of 100 nM and 1.2 μM respectively. Proteasome inhibitors are emerging as a new class of anticancer agents. MG132 inhibited the growth of HeLa cells via inducing the cell cycle arrest as well as triggering apoptosis. MG132 also inhibits NF-κB activation with an IC50 of 3 µM and prevents β-secretase cleavage. MG132 induces cell apoptosis through formation of reactive oxygen species or the upregulation and downregulation of these factors, which is ultimately dependent upon the activation of the caspase family of cysteine proteases. In vitro, it induces neurite outgrowth in PC12 cells and has anticancer properties. Besides its apoptotic effect alone, MG132 also enhanced the antiglioma effect of the chemotherapeutics cisplatin, taxol and doxorubicin in C6 and U138MG cells, indicating an adjuvant/chemosensitizer potential.