(S)-MG132
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.1,2 (S)-MG132 is a potent, reversible and cell permeable proteasome inhibitor that inhibits cell growth in B16 and IPC227F cells with IC50 values of 42 and 77 nM, respectively.3
133407-82-6 at 10 µM inhibits NF-κB activation, sensitizing a variety of carcinoma cell lines to apoptosis.4
Product Description References
1. Lee, D.H., and Goldberg, A.L. Proteasome inhibitors: Valuable new tools for cell biologists Trends in Cell Biology 8, 397-403 (1998).
2. Elliott, P.J., Zollner, T.M., and Boehncke, W.H. Proteasome inhibition: A new anti-inflammatory strategy Journal of Molecular Medicine 81, 235-245 (2003).
3. Vivier, M., Rapp, M., Papon, J., et al. Synthesis, radiosynthesis, and biological evaluation of new proteasome inhibitors in a tumor targeting approach Journal of Medicinal Chemistry 51(4), 1043-1047 (2008).
4. Arlt, A., Vorndamm, J., Breitenbroich, M., et al. Inhibition of NF- k B sensitizes human pancreatic carcinoma cells to apoptosis induced by etoposide (VP16) or doxorubicin Oncogene 20, 859-868 (2001).