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Epoxomicin | Irreversible 20S proteasome inhibitor

Epoxomicin (134381-21-8) is a potent, selective and cell permeable irreversible inhibitor of the 20S proteasome.1 It does not inhibit non-proteasomal proteases such as papain, chymotrypsin, trypsin, calpain and cathepsin B at concentrations up to 50 μM.1 Epoxomicin was isolated from Actinomycete strain Q996-17 and displayed in vivo antitumor activity against B16 melanoma cells.2 Epoxomicin caused a progressive model of Parkinson's disease in various systems.3,4,5 This model has been disputed.6,7

1) Meng et al. (1999), Epoxomicin, a potent and selective proteasome inhibitor, exhibits in vivo anti-inflammatory activity; Proc. Natl. Acad. Sci. USA, 96 10403
2) Hanada et al. (1992), Epoxomicin, a new antitumor agent of microbial origin; J. Antibiot. (Tokyo), 45 1746
3) McNaught et al. (2004), Systemic exposure to proteasome inhibitors causes a progressive model of Parkinson's disease; Ann. Neurol., 56 149
4) Matsui et al. (2010), Protesasome inhibition in medaka brain induces the features of Parkinson's disease; J. Neurochem., 115 178
5) Metcalfe et al. (2012), Coordination between proteasome impairment and caspase activation leading to TAU pathology:neuroprotection by cAMP; Cell Death Diff., 3 e326
6) Kordower et al. (2006), Failure of proteasome inhibitor administration to provide a model of Parkinson's disease in rats and monkeys; Ann. Neurol., 60 264
7) Bove et al. (2006), Proteasome inhibition and Parkinson's disease modeling; Ann. Neurol., 60 260

Focus Biomolecules supplier, chemical structure of Epoxomicin | Irreversible 20S proteasome inhibitor | CAS 134381-21-8

Catalog#  10-1384

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Catalog Number:
Irreversible 20S proteasome inhibitor
Molecular Weight:
Molecular Formula:
Soluble in DMSO (up to 10 mg/ml).
Physical Properties:
White solid
97% by HPLC
NMR (Conforms)
Storage Temperature:
Stable for 2 years as supplied. Solutions in DMSO may be stored at -20° for up to 2 months.
Shipping Code:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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