MG132 (133407-82-6) Description:

MG132 is a specific, potent, reversible, and cell-permeable proteasome inhibitor (Ki = 4 nM) . It reduces the degradation of ubiquitin-conjugated proteins in mammalian cells and permeable strains of yeast by the 26S complex without affecting its ATPase or isopeptidase activities. MG132 activates c-Jun N-terminal kinase (JNK1), which initiates apoptosis. MG132 also inhibits NF-κB activation with an IC50 of 3 µM and prevents β-secretase cleavage. MG-132 induces MCPIP1 expression; induces C6 glioma cell apoptosis via oxidative stress; induces AIF nuclear translocation through down-regulation of ERK and Akt/mTOR pathway.

MG-132 displays >1000 times more activity than ZLLal in inhibiting the ZLLL-MCA-degrading activity of 20S proteasome with IC50 of 100 nM versus 110 μM. MG-132 also inhibits calpain with IC50 of 1.2 μM. MG-132 induces neurite outgrowth in PC12 cells at an optimal concentration of 20 nM, displaying 500 times more potency than ZLLal.