Epoxomicin

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

Cell permeable: no

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

Product does not compete with ATP.

Reversible: no

Toxicity: Standard Handling (A)

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.

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.

Packaged under inert gas

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