Biochem/physiol Actions
Primary Target20S proteasome (MCP; multicatalytic proteinase complex)
Cell permeable: no
Reversible: no
Target IC50: 500 nM against 20S proteasome; 10 µM against NF-κB activation
Product does not compete with ATP.
General description
An irreversible proteasome inhibitor. A Streptomyces metabolite that acts as a highly specific inhibitor of the 20S proteasome (MCP; multicatalytic proteinase complex) (IC50 = 500 nM for 20S proteasome). Blocks proteasome activity by targeting the catalytic β-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 beyond theG1 phase of the cell cycle. Reported to induce apoptosis in human monoblast U937 cells. Also inhibits NF-κB activation (IC50 = 10 µM)
An irreversible proteasome inhibitor. A Streptomyces metabolite that acts as a highly specific inhibitor of the 20S proteasome (MCP; multicatalytic proteinase complex) (IC50 = 500 nM for 20S proteasome). Blocks proteasome activity by targeting the catalytic β-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-κB activation (IC50 = 10 µM).
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Other Notes
Keyomarsi, K., et al. 2011. Cell. Biol. Toxicol.27, 123.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. Science268, 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. USA91, 3358.Omura, S., et al. 1991. J. Antibiot.44, 117.
Packaging
1 mg in Glass bottle
200, 400 µg in Plastic ampoule
Reconstitution
Following reconstitution in DMSO, aliquot and freeze (-20°C). DMSO stock solutions are stable for up to 1 month at -20°C. Unstable in aqueous solutions; reconstitute in H2O just prior to use.
Warning
Toxicity: Standard Handling (A)
This product has met the following criteria to qualify for the following awards: