MG-132
Proteasome inhibitor / 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-autophagy2. Activates stress kinases and induces Hsp72.3 Induces neurite outgrowth.1 Blocks NFκB activation by blocking IκB proteolysis (IC50=3 μM).4 Cell permeable.
Biochemicals & reagents
133407-82-6
Z-Leu-Leu-Leu-CHO
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
-20°C
TARGET: Proteasome -- PATHWAY: Degradation; NFkappaB; Proliferation; Autophagy; Cytokine -- RESEARCH AREA: Ubiquitin/Proteasome; Cell death; Stem cells -- DISEASE AREA: Cancer; DiabetesInflammation; Heart disease