MG-132 is a cell permeable reversible proteosome inhibitor. MG-132 is also called as carbobenzoxy-L-leucyl-L-leucyl-L-leucinal, Z-LLL-CHO, is a peptide aldehyde, part of a group of chemicals capable of inhibiting proteases, such as serine proteases and calpain etc. MG-132 reduces the degradation of IκB (inhibitory κB), GRK2 (G-protein-receptor kinase 2), ARC (apoptosis repressor with caspase recruitment domain), and HSP (heat shock proteins), all of which exert beneficial effects on acute myocardial ischemia. Moderate proteasome inhibition by MG132 results in the upregulation of anti-oxidative enzymes, and it protects rat myocytes against H₂O₂-mediated oxidative stress. It also inhibits 5-lipoxygenase that selectively disrupts function of c-Myc in cancer cells and NF- κB activation.

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