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Epoxomicin

Key inhibitor for use in proteasome research.
 
BML-PI127-0100 100 µg 184.00 USD
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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
 
CAS:134381-21-8
 
MI:14: 3630
 
Purity:≥95% (HPLC)
 
Appearance:Lyophilized. Very thin transparent film.
 
Solubility:Soluble in DMSO (15mg/ml) or dichloromethane:methanol (9:1); insoluble in water.
 
Shipping:Shipped on Blue Ice
 
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:Protect from light. Avoid freeze/thaw cycles.
 
ALX-350-254
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ALX-350-254

Product Literature References

Caspase vinyl sulfone small molecule inhibitors prevent axonal degeneration in human neurons and reverse cognitive impairment in Caspase-6-overexpressing mice: P. Pakavathjkumar, et al.; Mol. Neurodegener. 12, 22 (2017), Abstract; Full Text
Comparative Proteomics Reveals Strain-Specific β-TrCP Degradation via Rotavirus NSP1 Hijacking a Host Cullin-3-Rbx1 Complex: S. Ding, et al.; PLoS Pathology 12, e1005929 (2016), Application(s): Cell treatment, Abstract; Full Text
Prion-mediated neurodegeneration is associated with early impairment of the ubiquitin-proteasome system: C. McKinnon, et al.; Acta Neuropathol. 131, 411 (2016), Application(s): Determined background activity caused by non-proteasomal degradation, Abstract; Full Text
Bortezomib Amplifies Effect on Intracellular Proteasomes by Changing Proteasome Structure: D.S. Pitcher, et al.; EBioMedicine 2, 642 (2015), Application(s): Western Blot, Abstract;
The regulation of glucose on milk fat synthesis is mediated by the ubiquitin-proteasome system in bovine mammary epithelial cells: L. Liu, et al.; Biochem. Biophys. Res. Commun. 465, 59 (2015), Application(s): Cell culture, Abstract;
The small heat shock protein B8 (HSPB8) confers resistance to bortezomib by promoting autophagic removal of misfolded proteins in multiple myeloma cells: M. Hamouda, et al.; Oncotarget 5, 6252 (2014), Application(s): Analysis of velcade resistant multiple myeloma human cells by WB, Assay, Abstract; Full Text
Pathogen signatures activate a ubiquitination pathway that modulates the function of the metabolic checkpoint kinase mTOR: S. Ivanov & C. Roy; Nat. Immunol. 14, 1219 (2013), Application(s): Analysis of mouse macrophages by WB, PCR, Abstract; Full Text
Removal of damaged proteins during ES cell fate specification requires the proteasome activator PA28: M. Hernebring, et al.; Sci. Rep. 3, 1381 (2013), Abstract; Full Text
Protein carbonylation and aggregation precede neuronal apoptosis induced by partial glutathione depletion: A. Dasgupta, et al.; ASN Neuro 4, e00084 (2012), Abstract; Full Text
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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