| Description | MG-132 (133407-82-6) is a 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 MG-132 blocks NFκB activation by blocking IκB proteolysis (IC50=3 μM).4 Cell permeable. |
| Uses | A proteasome and NF-κB inhibitor. |
| Uses | MG 132 is a potent, membrane-permeable proteasome inhibitor. It induces neurite outgrowth in PC12 cells. Neuroprotective product. |
| Definition | ChEBI: A tripeptide that is L-leucyl-L-leucyl-L-leucine in which the C-terminal carboxy group has been reduced to the corresponding aldehyde and the N-terminal amino group is
protected as its benzyloxycarbonyl derivative. |
| General Description | Potent, reversible, and cell-permeable proteasome inhibitor (Ki = 4 nM). Reduces the degradation of ubiquitin-conjugated proteins in mammalian cells and permeable stains of yeast by the 26S complex without affecting its ATPase or isopeptidase activities. Activates c-Jun N-terminal kinase (JNK1) and inhibits NF-κB activation (IC50 = 3 μM). |
| Biological Activity | Potent cell-permeable inhibitor of proteasome (IC 50 = 100 nM) and calpain (IC 50 = 1.2 μ M). Inhibits TNF- α -induced NF- κ B activation and I κ B α degradation. Induces neurite outgrowth in PC12 cells and has anticancer properties in vitro . |
| Biochem/physiol Actions | Cell permeable: yes |
| storage | -20°C (desiccate) |
| 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 |
