MG-132 #2194

MG-132 is a potent proteasome and calpain inhibitor. Research studies have shown that MG-132 prevents degradation of the proteasome substrates SucLLVY-MCA and ZLLL-MCA with an IC₅₀ of 850 nM and 100 nM, respectively, as well as inhibits casein-degrading activity of m-calpain with an IC₅₀ of 1.25 µM (1). Investigators have demonstrated that MG-132 inhibits TNF-α-induced NF-κB activation and IL-8 release in A549 cells (2). Proteasome inhibition with MG-132 prevents degradation of short-lived proteins, which correlates with increased expression of HSP and ER chaperone proteins (3). MG-132 induces apoptosis in Hep G2 cells in a time- and dose-dependent manner (4). Proteasome inhibitors like MG-132 are important research tools for studying cellular degradation of the ubiquitin-proteasome pathway.