Epoxomicin

• 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.

• Description :

  Proteasome inhibitor

• CAS Number :

  134381-21-8

• 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

• Type :

  Inhibitor

• Source :

  Synthetic

• Field of Research :

  Cell Signaling

• 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.