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Epoxomicin Chemical Structure

Epoxomicin

Data Sheet For research use only. Not for human use.
Cat. No. :BCP13740CAS No. :134381-21-8Purity:98%
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  • Chemical Properties&Biological Activity
CAS No. 134381-21-8 Cat. No. BCP13740
Name Epoxomicin
Synonyms BU-4061T;
SMILES O=C([C@@H](NC([C@H]([C@@H](C)O)NC([C@@H](NC([C@H]([C@@H](C)CC)N(C)C(C)=O)=O)[C@@H](C)CC)=O)=O)CC(C)C)[C@@]1(C)CO1
Chemical Name
Formula C28H50N4O7 M. Wt 554.72
Purity 98% Storage Store at 4-8°C
Description Epoxomicin is a potent anti-tumor agent isolated from Actinomycetes that is used as a selective and irreversible inhibitor of the 20S proteasome. It inhibits proteasome activity in cell growth assays with an IC50 value of 4 nM and demonstrates potent cytotoxicity against B16-F10, HCT116, and Moser solid tumor cells, as well as P388 and K562 leukemia cells with IC50 values ranging from 2-44 nM. By inhibiting osteoblast proteasome activity, epoxomicin stimulates bone formation at concentrations as low as 10 nM. Intraperitoneal injection of 1.5 mg/kg epoxomicin given daily for two weeks induces Parkinson's-like symptoms in rats and addition of 100 nM epoxomicin to rat ventral midbrain cultures results in apoptosis specific to dopaminergic neurons. Epoxomicin-induced parkinsonism can be a useful model to examine mechanisms and therapies for the disease.
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