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 |
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| MW: | 554.7 |
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| Purity: | ≥95% (HPLC) |
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| Appearance: | White solid. |
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| CAS: | 134381-21-8 |
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| MI: | 14: 3630 |
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| Solubility: | Soluble in DMSO (15mg/ml) or dichloromethane:methanol (9:1); insoluble in water. |
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| Long Term Storage: | -20°C |
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| 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. |
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| Handling: | Avoid freeze/thaw cycles. Protect from light. |
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| Background / Technical Information: | Please click here for the comprehensive product datasheet. |
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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;