Manumycin A

Manumycin A

CAT N°: 10010497
Price:

From €166.00 €141.10

Manumycin A is an antibiotic that acts as a potent and selective farnesyltransferase (FTase) inhibitor with anti-tumor activity.{15668,15667} It inhibits rat brain FTase with a Ki value of 1.2 µM, thereby preventing Ras activation which requires farnesylation at the C-terminus for membrane attachment.{15668} It exhibits significant antitumor activity against Ki-ras-activated solid tumors in mice at a dose of 6.3 mg/kg.{15668} Manymycin A inhibits I?B kinase (IKK), independent of FTase inhibition, in an number of cells types with effective concentrations of 2-10 µM.{15666} In ApoE-deficient mice, Manumycin A treatment for 22 weeks at 5 mg/kg reduced aortic fatty streak lesion size to 43% of vehicle-treated animals, indicating FTase inhibition as a potential target for prevention or treatment of atherosclerosis.{15035}

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • N-[(1S,5S,6R)-5-hydroxy-5-[(1E,3E,5E)-7-[(2-hydroxy-5-oxo-1-cyclopenten-1-yl)amino]-7-oxo-1,3,5–heptatrien-1-yl]-2-oxo-7-oxabicyclo[4.1.0]hept-3-en-3-yl]-2E,4E,6R-trimethyl,2,4-decadienamide
  • Correlated keywords
    • farnesyltransferase inhibitors inhibits inhibition cancer antitumor anti-tumor signal transduction Ras farnesylation NF-.kappa.B NF-kB NF-kappaB protein lipidation
  • Product Overview:
    Manumycin A is an antibiotic that acts as a potent and selective farnesyltransferase (FTase) inhibitor with anti-tumor activity.{15668,15667} It inhibits rat brain FTase with a Ki value of 1.2 µM, thereby preventing Ras activation which requires farnesylation at the C-terminus for membrane attachment.{15668} It exhibits significant antitumor activity against Ki-ras-activated solid tumors in mice at a dose of 6.3 mg/kg.{15668} Manymycin A inhibits I?B kinase (IKK), independent of FTase inhibition, in an number of cells types with effective concentrations of 2-10 µM.{15666} In ApoE-deficient mice, Manumycin A treatment for 22 weeks at 5 mg/kg reduced aortic fatty streak lesion size to 43% of vehicle-treated animals, indicating FTase inhibition as a potential target for prevention or treatment of atherosclerosis.{15035}

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