Epoxomicin solution (CAS 134381-21-8)
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Epoxomicin is a potent proteasome inhibitor, primarily inhibiting the chymotrypsin-like activity of the proteasome. The novel α-epoxy ketone moiety of Epoxomicin forms covalent bonds with residues in particular catalytic subunits of the enzyme, disabling activity. The trypsin-like and peptidyl-glutamyl peptide hydrolyzing behavior of the proteasome were both inhibited by Epoxomicin as well (at 100 and 1,000-fold slower rates, respectively). Bone formation is heavily regulated by the ubiquitin-proteasome pathway, and Epoxomicin was shown to increase both bone volume and bone formation rates in rodents. Another study demonstrates that exposure to Epoxomicin and other proteasome inhibitors leads to dopaminergic cell death, producing a model of Parkinson′s disease in vivo.
Epoxomicin solution (CAS 134381-21-8) References
- Epoxomicin, a potent and selective proteasome inhibitor, exhibits in vivo antiinflammatory activity. | Meng, L., et al. 1999. Proc Natl Acad Sci U S A. 96: 10403-8. PMID: 10468620
- The selective proteasome inhibitors lactacystin and epoxomicin can be used to either up- or down-regulate antigen presentation at nontoxic doses. | Schwarz, K., et al. 2000. J Immunol. 164: 6147-57. PMID: 10843664
- Cells adapted to the proteasome inhibitor 4-hydroxy- 5-iodo-3-nitrophenylacetyl-Leu-Leu-leucinal-vinyl sulfone require enzymatically active proteasomes for continued survival. | Princiotta, MF., et al. 2001. Proc Natl Acad Sci U S A. 98: 513-8. PMID: 11149939
- Selective inhibitors of the osteoblast proteasome stimulate bone formation in vivo and in vitro. | Garrett, IR., et al. 2003. J Clin Invest. 111: 1771-82. PMID: 12782679
- Epoxomicin, a new antitumor agent of microbial origin. | Hanada, M., et al. 1992. J Antibiot (Tokyo). 45: 1746-52. PMID: 1468981
- Systemic exposure to proteasome inhibitors causes a progressive model of Parkinson's disease. | McNaught, KS., et al. 2004. Ann Neurol. 56: 149-62. PMID: 15236415
- Estrogen suppresses uterine epithelial apoptosis by inducing birc1 expression. | Yin, Y., et al. 2008. Mol Endocrinol. 22: 113-25. PMID: 17901126
- Human Metapneumovirus Escapes NK Cell Recognition through the Downregulation of Stress-Induced Ligands for NKG2D. | Diab, M., et al. 2020. Viruses. 12: PMID: 32698530
- An antibody-based amperometric biosensor for 20S proteasome activity and inhibitor screening. | Barsan, MM. and Diculescu, VC. 2021. Analyst. 146: 3216-3224. PMID: 33999049
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
Epoxomicin solution, 100 µg | sc-363786 | 100 µg | $270.00 |