(R)-MG-132 is a potent, reversible and cell permeable proteasome inhibitor. The ubiquitin-proteasome pathway plays an integral role in the selective degradation of intracellular proteins. While important for clearing damaged or misfolded proteins, this proteolytic pathway also regulates the availability of key proteins involved in the control of inflammatory processes, cell cycle regulation, and gene expression. After treatment for one hour at 100 nM, (R)-MG-132 inhibits 50% and 31% of proteasome activity in lysates of J558L multiple myeloma cells and EMT6 breast cancer cells, respectively. The (R)-MG-132 stereoisomer is a more effective inhibitor of chymotrypsin-like (ChTL), trypsin-like (TL), and peptidylglutamyl peptide hydrolyzing proteasome (PGPH) activities compared to (S)-MG-132 (IC50 = 0.22 µM versus 0.89 µM (ChTL); 34.4 µM versus 104.43 µM (TL); 2.95 µM versus 5.70 µM (PGPH), respectively).
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See how others have used (R)-MG-132. Click on the entry to view the PubMed entry .
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