Biochem/physiol Actions

Primary TargetCT-L,T-L,PGPH activity of proteasome

Cell permeable: no

Reversible: no

Product does not compete with ATP.

General description

An antitumor agent of microbial origin that acts as a potent, highly specific, and irreversible inhibitor of chymotrypsin-like (CT-L), trypsin-like (T-L), and peptidylglutamyl peptide hydrolyzing (PGPH) activities of the proteasome. Modifies the proteasomal catalytic subunits LMP-7, MECL1, and Z. Epoxomicin also displays potent anti-inflammatory activity in vivo.

An antitumor and anti-inflammatory agent that acts as a potent, highly specific, and irreversible inhibitor of chymotrypsin-like (CT-L), trypsin-like (T-L), and peptidyl-glutamyl peptide hydrolyzing (PGPH) activities of the proteasome. Modifies the proteasomal catalytic subunits LMP-7, MECL1, and Z. Does not affect the activities of non-proteasomal proteases such as trypsin, cathepsin B, or chymotrypsin. A 1 mM (50 µg/90 µl) solution of Epoxomicin, Synthetic (Cat. No. 324801) in DMSO is also available.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Meng, L., et al. 1999. Proc. Natl. Acad. Sci. USA 96, 10403.Sin, N., et al. 1999. Bioorg. Med. Chem. Lett. 9, 2283.Hanada, M., et al. 1992. J. Antibiot. 45, 1746.

Packaging

Packaged under inert gas

100 µg in Glass bottle

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

Warning

Toxicity: Standard Handling (A)