Epoxomicin

Proteasome inhibitor

Product Specifications

Background

Epoxomicin is a cell permeable, potent and selective proteasome inhibitor originally isolated from Actinomycetes strain based on its potent in vivo antitumor activity. It is a more potent inhibitor of the chymotrypsin-like activity of the proteasome than lactacystin. Epoxomicin also blocks trypsin-like and PGPH activities of the proteasome and regulates antigen presentation at non-toxic doses. It effectively inhibits NF-κB activation in vitro and potently blocks inflammation in vivo in the mouse ear edema assay. The ubiquitin-proteasome system (UPS) and autophagy serve as two complementary, reciprocally regulated protein degradation systems, thus inhibition of UPS by Epoxomicin activates autophagy.

Product Name Alternative

N-Acetyl-N-methyl-L-isoleucyl-L-isoleucyl-N-[(1S)-3-methyl-1-[[(2R)-2-methyloxiranyl]carbonyl]butyl]-L-threoninamide

UNSPSC

41116105

Source

Synthetic

Purity

>95%

Weight

0.0001

Format

White solid

Solubility

Soluble in DMSO (15 mg/ml) or dichloromethane:methanol (9:1); insoluble in water.

Molecular Formula

C28H50N4O7

Molecular Weight

554.7

Precautions

Not for use in humans. Not for use in diagnostics or therapeutics. For in vitro research use only.

References & Citations

1. F. Yang, et al. (2009) Neurosci. Lett. 454: 203. 2. K. Ohkawa, et al. (2004) Int. J. Oncol. 24: 425. 3. K. Schwarz, et al. (2000) J. Immunol. 164: 6147. 4. L. Meng, et al. (1999) PNAS. 96: 10403. 5. K.B. Kim, et al. (1999) Bioorg. Med. Chem. Lett. 9: 3335. 6. N. Sin, et al. (1999) Bioorg. Med. Chem. Lett. 9: 2283. 7. M. Hanada, et al. (1992) J. Antibiot. (Tokyo) 45: 1746.