AG-CN2-0422-C05050 µgCHF 90.00
AG-CN2-0422-C100100 µgCHF 150.00
AG-CN2-0422-C250250 µgCHF 290.00
AG-CN2-0422-C500500 µgCHF 450.00
|Synonyms||Antibiotic BU 4061T|
|Merck Index||14: 3630|
|Purity Chemicals||≥97% (NMR)|
|Appearance||White to off-white solid.|
|Solubility||Soluble in DMSO. Insoluble in water.|
|Shipping and Handling|
|Short Term Storage||+4°C|
|Long Term Storage||-20°C|
Keep cool and dry.
Protect from light and moisture.
|Use/Stability||Stable for at least 2 years after receipt when stored at -20°C.|
|Product Specification Sheet|
- Antibiotic .
- Potent anticancer compound [1, 7].
- Cell permeable, potent, selective and irreversible 20S proteasome inhibitor. Predominantly inhibits the chymotrypsin-like (CTRL) activity of the proteasome. Exhibits lower level inhibition of proteasome trypsin-like and caspase-like activitives (100 and 1,000-fold slower rates respectively) [2, 3].
- Anti-inflammatory .
- Antimicrobial and antimalarial .
- Anti-parasitic .
- Stimulates bone formation by inhibiting osteoblast proteasome activity .
- Induces Parkinson's-like symptoms in rats .
- The ubiquitin-proteasome system (UPS) and autophagy serve as two complementary, reciprocally regulated protein degradation systems. Blockade of UPS by Epoxomicin activates autophagy.
- Blocks the Thymoproteasome β5t subunit activity.
- Epoxomicin, a new antitumor agent of microbial origin: M. Hanada, et al.; J. Antibiot. 45, 1746 (1992)
- Total synthesis of the potent proteasome inhibitor epoxomicin: a useful tool for understanding proteasome biology: N. Sin, et al.; Bioorg. Med. Chem. Lett. 9, 2283 (1999)
- Proteasome inhibition by the natural products epoxomicin and dihydroeponemycin: insights into specificity and potency: K.B. Kim, et al.; Bioorg. Med. Chem. Lett. 9, 3335 (1999)
- Epoxomicin, a potent and selective proteasome inhibitor, exhibits in vivo antiinflammatory activity: L. Meng, et al.; PNAS 96, 10403 (1999)
- Selective inhibitors of the osteoblast proteasome stimulate bone formation in vivo and in vitro: I.R. Garrett, et al.; J. Clin. Invest. 111, 1771 (2003)
- Systemic exposure to proteasome inhibitors causes a progressive model of Parkinson's disease: K.S. McNaught, et al.; Ann. Neurol. 56, 149 (2004)
- Establishment and some characteristics of epoxomicin (a proteasome inhibitor) resistant variants of the human squamous cell carcinoma cell line, A431: K. Ohkawa, et al.; Int. J. Oncol. 24, 425 (2004)
- The proteasome inhibitor epoxomicin has potent Plasmodium falciparum gametocytocidal activity: B. Czesny, et al.; Antimicrob. Agents Chemother. 53, 4080 (2009)
- Evaluation of the in vitro growth-inhibitory effect of epoxomicin on Babesia parasites: M. Aboulaila, et al.; Vet. Parasitol. 167, 19 (2010)
- Mechanisms of cross-talk between the ubiquitin-proteasome and autophagy-lysosome systems: V.I. Korolchuk, et al.; FEBS Lett. 584, 1393 (2010)
- Activity-Based Profiling Reveals Reactivity of the Murine Thymoproteasome-Specific Subunit β5t: B.I. Florea, et al.; Chem. Biol. 17, 795 (2010)