(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).
Related products include the S conformer, MG-132 [Z-Leu- Leu-Leu-CHO] (sc-201270).
1. Lee, D.H. and Goldberg, A.L. 1998. Trends Cell Biol. 8: 397-403. PMID: 9789328
2. Arlt, A., et al. 2001. Oncogene. 20: 859-868. PMID: 11314019
3. Elliott, P.J., et al. 2003. J. Mol. Med. 81: 235-245. PMID: 12700891
4. Vivier, M., et al. 2008. J. Med. Chem. 51: 1043-1047. PMID: 18237109
See how others have used (R)-MG-132. Click on the entry to view the PubMed entry .
PMID: # 28086019 Haidar, M. et al. 2017. ACS Infect Dis. 3: 216-224.
PMID: # 25927990 Amaya, M. et al. 2015. PLoS ONE. 10: e0124792.
PMID: # 26250624 Jewett, K. et al. 2015. J Neurochem.
PMID: # 24608790 Peuget, S. et al. 2014. Cell Death Differ. 21: 1107-18.
PMID: # 23319609 Yang, F. et al. 2013. Proc. Natl. Acad. Sci. U.S.A. 110: 1863-8.
PMID: # 22461906 Lazar, C. et al. 2012. PloS one. 7: e34169.
Santa Cruz Biotechnology, Inc. is a world leader in the development of products for the biomedical research market. Call us Toll Free at 1-800-457-3801.
Copyright © 2007-2019 Santa Cruz Biotechnology, Inc. All Rights Reserved. "Santa Cruz Biotechnology", and the Santa Cruz Biotechnology, Inc. logo, "Santa Cruz Animal Health", "San Juan Ranch", "Supplement of Champions", the San Juan Ranch logo, "Ultracruz", "Chemcruz", "Immunocruz", "Exactacruz", and "EZ Touch" are registered trademarks of Santa Cruz Biotechnology, Inc.
All trademarks are the property of their respective owners.