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Epoxomicin

Key inhibitor for use in proteasome research.
 
BML-PI127-0100 100 µg 183.00 USD
 
Replaces Prod. #: ALX-350-254

Cell permeable, potent and selective proteasome inhibitor originally isolated from Actinomycetes strain based on its potent in vivo antitumor activity. More potent inhibitor of the chymotrypsin-like activity of the proteasome than lactacystin (Prod. No. BML-PI104). Blocks also trypsin-like and PGPH activities of the proteasome. Regulates antigen presentation at non-toxic doses. 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 blockade of UPS by Epoxomicin activates autophagy.

Product Specification

Formula:C28H50N4O7
 
MW:554.7
 
Purity:≥95% (HPLC)
 
Appearance:White solid.
 
CAS:134381-21-8
 
MI:14: 3630
 
Solubility:Soluble in DMSO (15mg/ml) or dichloromethane:methanol (9:1); insoluble in water.
 
Long Term Storage:-20°C
 
Use/Stability:Stable for at least 1 year after receipt when stored, as supplied, at -20°C. Stock solutions are stable for up to 3 months at -20°C.
 
Handling:Avoid freeze/thaw cycles.
Protect from light.
 
Background / Technical Information:Please click here for the comprehensive product datasheet.
 
ALX-350-254
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ALX-350-254

Product Literature References

Role of autophagy and proteasome degradation pathways in apoptosis of PC12 cells overexpressing human alpha-synuclein: F. Yang, et al.; Neurosci. Lett. 454, 203 (2009), Abstract;
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), Abstract;
The selective proteasome inhibitors lactacystin and epoxomicin can be used to either up- or down-regulate antigen presentation at nontoxic doses: K. Schwarz, et al.; J. Immunol. 164, 6147 (2000), Abstract;
Epoxomicin, a potent and selective proteasome inhibitor, exhibits in vivo antiinflammatory activity: L. Meng, et al.; PNAS 96, 10403 (1999), Abstract;
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), Abstract;
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), Abstract;
Epoxomicin, a new antitumor agent of microbial origin: M. Hanada, et al.; J. Antibiot. (Tokyo) 45, 1746 (1992), Abstract;

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