Epoxomicin

Cell permeable: No


Product does not compete with ATP.


Reversible: No

Epoxomicin is a highly effective and selective proteasome inhibitor thatexhibits significant anti-inflammatory properties in vivo. This potent antitumor agent specifically targets the proteasome. Epoxomicin exhibits a stronger inhibitory effect on chymotrypsin-like activity compared to lactacystin and the peptide vinyl sulfone (NLVS). This powerful natural producteffectively inhibits nuclear factor kappa B (NF-κB) activation in vitro and signific antly reduces inflammation in the murine ear edema assay. Epoxomicin prevents the degradation of IκB and inhibits the activation of NF-κBDNA-binding activity. It can stabilize p53 levels in cell culture. It is an irreversible inhibitor of chymotrypsin-like (CT-L), trypsin-like (T-L), and peptidylglutamyl peptide hydrolyzing (PGPH) activities of the proteasome. It modifies the proteasomal catalytic subunits LMP-7, MECL1, and Z[MJ2] .

Epoxomicin has been used incell culture for proteasome inhibition experiments. It has also been used incell culture medium to treat MODE-K cells for stimulation to blockproteasome.

Packaged under inert gas

A 1 mM (50 µg/90 µl) solution of Epoxomicin, Synthetic (Cat. No. 324800) in DMSO.

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

Toxicity: Irritant (B)