A potent and selective farnesyltransferase (FTase) inhibitor with anti-tumor activity: inhibits rat brain FTase with a Ki value of 1.2 µM

Manumycin A – 1 mg

Brand:
Cayman
CAS:
52665-74-4
Storage:
-20
UN-No:
Non-Hazardous - /

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 IκB 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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SKU: 10010497 - 1 mg Category:

Description

A potent and selective farnesyltransferase (FTase) inhibitor with anti-tumor activity: inhibits rat brain FTase with a Ki value of 1.2 µM, thereby preventing Ras activation; inhibits IKK in an number of cells types

Formal name: 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

Synonyms:  NSC 622141|UCF 1C

Molecular weight: 550.7

CAS: 52665-74-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|IKKs||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|GTPases||Research Area|Cancer|Cell Signaling|NF-κB Signaling||Research Area|Cancer|Transcription Factors|NF-κB||Research Area|Cardiovascular System|Cardiovascular Diseases|Atherosclerosis||Research Area|Immunology & Inflammation

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