Epoxomicin is a linear peptide consisting of a threonine or serine residue with α ′, β′-epoxyketone derived from leucine or a γ, δ-dehydroleucine. It is a natural product isolated from Actinomyces sp., And is a potent, selective, and irreversible cell-permeable proteasome inhibitor.
Epoxomicin has been used:
- as an inhibitor of the ubiquitin-proteasome system (UPS) in pheochromocytoma PC12 cells.
- as a proteasome inhibitor in mammary epithelial MCF-10A cells.
- as a proteasome inhibitor in chymotryptic assays in cardiomyocytes.
Packaging: 50 μg in a glass bottle
Biochemical / Physiological Actions
Epoxomicin binds covalently to the catalytic subunits of the proteasome. It forms an adduct with target proteins. Inhibits the chymotrypsin-like activity of the proteasome. Epoxomicin also inhibits activated B-cell light chain enhancer nuclear factor κ (NF-κB) mediated by the proinflammatory signaling pathway. It is also a powerful anti-tumor and anti-inflammatory agent. Epoxomicin, a natural product isolated from Actinomyces sp., Is a potent, selective, and irreversible cell-permeable proteasome inhibitor.