Reagenti e strumenti per immunologia, biologia cellulare e biologia molecolare
 
> Epoxomicin

Epoxomicin

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Cat# 226810-250ug

Size : 250ug

Marca : US Biological


226810 Epoxomicin

Grade
Highly Purified
Shipping Temp
RT
Storage Temp
-20°C

Antibiotic. Potent anticancer compound. 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). 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.

Alternate Names:
N-acetyl-N-methyl-L-isoleucyl-L-isoleucyl-N-[(1S)-3-methyl-1-[[(2R)-2-methyloxiranyl]carbonyl]butyl]-L-threoninamide, BU 4061T

CAS Number:
134381-21-8

Source:
Synthetic

Molecular Formula:
C₂₈H₅₀N₄O₇

Molecular Weight:
554.7

Solubility:
Soluble in DMSO. Insoluble in water.

Purity:
≥97% (NMR)

Appearance:
Supplied as a white to off-white solid.

Storage and Stability:
Stable for 1 year after receipt when stored at -20°C. Keep cool and dry. Protect from light and moisture.

Important Note:
This product as supplied is intended for research use only, not for use in human, therapeutic or diagnostic applications without the expressed written authorization of United States Biological.

Toxicity and Hazards: 
All products should be handled by qualified personnel only, trained in laboratory procedures.

Applications
Source: Synthetic|Purity: ≥97% (NMR) |Form: Supplied as a white to off-white solid. ||Important Note: This product as supplied is intended for research use only, not for use in human, therapeutic or diagnostic applications without the expressed written authorization of United States Biological.
Form
Supplied as a white to off-white solid.
Purity
≥97% (NMR)
References
1. Epoxomicin, a new antitumor agent of microbial origin: M. Hanada, et al.; J. Antibiot. 45, 1746 (1992). 2. 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). 3. 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). 4. Epoxomicin, a potent and selective proteasome inhibitor, exhibits in vivo antiinflammatory activity: L. Meng, et al.; PNAS 96, 10403 (1999). 5. 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). 6. Systemic exposure to proteasome inhibitors causes a progressive model of Parkinson's disease: K.S. McNaught, et al.; Ann. Neurol. 56, 149 (2004). 7. 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). 8. The proteasome inhibitor epoxomicin has potent Plasmodium falciparum gametocytocidal activity: B. Czesny, et al.; Antimicrob. Agents Chemother. 53, 4080 (2009). 9. Evaluation of the in vitro growth-inhibitory effect of epoxomicin on Babesia parasites: M. Aboulaila, et al.; Vet. Parasitol. 167, 19 (2010). 10. Mechanisms of cross-talk between the ubiquitin-proteasome and autophagy-lysosome systems: V.I. Korolchuk, et al.; FEBS Lett. 584, 1393 (2010).