White solid. An irreversible proteasome inhibitor. A Streptomyces metabolite that acts as a highly specific inhibitor of the 20S proteasome (MCP; multicatalytic proteinase complex). Blocks proteasome activity by targeting the catalytic b-subunit. Acts as a covalent inhibitor of the chymotrypsin- and trypsin-like activities of the proteasome. Induces neurite outgrowth in Neuro 2A mouse neuroblastoma cells and inhibits progression of synchronized Neuro 2A cells and MG-63 human osteosarcoma cells beyond the G1 phase of the cell cycle. Reported to induce apoptosis in human monoblast U937 cells. Also inhibits NF-kB activation (IC50 = 10 µM). Purity: Purity by HPLC.. Ref.: Adams, J., and Stein, R. 1996. Ann. Rep. Med. Chem. 31, 279. Dick, L.R., et al. 1996. J. Biol. Chem. 271, 7273. Oda, K., et al. 1996. Biochem. Biophys. Res. Commun. 219, 800. Fenteany, G., et al. 1995. Science 268, 726. Imajoh-Ohmi, S., et al. 1995. Biochem. Biophys. Res. Commun. 217, 1070. Jensen, T.J., et al. 1995. Cell 83, 129. Katagiri, M.M., et al. 1995. J. Antibiot. 48, 344. Mori, S., et al. 1995. J. Biol. Chem. 270, 29447. Tanaka, H., et al. 1995. Biochem. Biophys. Res. Commun. 216, 291. Fenteany, G., et al. 1994. Proc. Natl. Acad. Sci. USA 91, 3358. Omura, S., et al. 1991. J. Antibiot. 44, 117. |
