Epoxomicin

Epoxomicin

CAT N°: 10007806
Price:

From 94.00 79.90

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.{13359,13358} By inhibiting osteoblast proteasome activity, epoxomicin stimulates bone formation at concentrations as low as 10 nM.{13351} 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.{13355,16504} Epoxomicin-induced parkinsonism can be a useful model to examine mechanisms and therapies for the disease.

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • N-acetyl-N-methyl-L-isoleucyl-L-isoleucyl-N-[(1S)-3-methyl-1-[[(2R)-2-methyloxiranyl]carbonyl]butyl]-L-threoninamide
  • Correlated keywords
    • inhibitors inhibits inhibition proteins degradation 20S proteasomes antitumors bones formation Parkinsons diseases anti-tumors
  • Product Overview:
    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.{13359,13358} By inhibiting osteoblast proteasome activity, epoxomicin stimulates bone formation at concentrations as low as 10 nM.{13351} 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.{13355,16504} Epoxomicin-induced parkinsonism can be a useful model to examine mechanisms and therapies for the disease.

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