Epoxomicin

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.

Cell permeable: no

Primary Target
CT-L,T-L,PGPH activity of proteasome

Product does not compete with ATP.

Reversible: no

Packaged under inert gas

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

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.

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

Toxicity: Standard Handling (A)