MG-132

Specific inhibitor of the chymotrypsin-like activity of the 20S proteasome (IC50=100 nM with Z-LLL-AMC as substrate) [1]. Also inhibits calpain (IC50=1.25 μM) [1]. Suppresses gastric cancer cell proliferation and induces macro-autophagy [2]. Activates stress kinases and induces Hsp72 [3]. Induces neurite outgrowth [1]. Blocks NFκB activation by blocking IκB proteolysis (IC50=3 μM) [4]. Cell permeable.

References:

1) Tsubuki et al. (1996), Differential inhibition of calpain and proteasome activities by peptidyl aldehydes of di-leucine and tri-leucine ; J. Biochem.,  119 572

2) Wu  et al. (2010), Macroautophagy and ERK phosphorylation counteract the antiproliferative effect of proteasome inhibitor in gastric cancer cells; Autophagy, 6 228

3) Meriin  et al. (1998), Proteasome inhibitors activate stress kinases and induce Hsp72. Diverse effects on apoptosis; J. Biol. Chem., 273 6373

4) Fiedler et al. (1998), 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., 19 259