|FTI 277 HClFTase inhibitor|
Sample solution is provided at 25 µL, 10mM.
Publications citing ApexBio Products
|Cas No.||180977-34-8||SDF||Download SDF|
|Chemical Name||(Z)-5-(((R)-2-amino-3-mercaptopropyl)amino)-N-((S)-1-methoxy-4-(methylthio)-1-oxobutan-2-yl)-[1,1'-biphenyl]-2-carbimidic acid hydrochloride|
|Solubility||Soluble in DMSO||Storage||Store at -20°C|
FTI-277 is a highly potent and selective FTase inhibitor. At concentration as low as 10 nM, FTI-277 inhibits H-Ras processing and the processing is blocked by more than 95% at 3 μM. 
Ras proteins are plasma membrane-associated GTPases. It acts as relay switches transducing biological information from extracellular signals to the nucleus. Farnesyltransferase (FTase) is an enzyme that catalyzed the Ras farnesylation, a lipid posttranslational modification that is required for Ras-induced malignant transformation. 
FTI-277, the methyl ester derivative of FTI-276, is extremely potent (ICGraphic = 100 nM) at inhibiting H-Ras, but not the geranylgeranylated Rap1A processing in whole cells. FTI-277 is a farnesylation-specific inhibitor which inhibits the processing of both oncogenic and normal Ras. 
In mice that hydrodynamically transfected to produce Hepatitis delta virus (HDV) viremia, FTI-277 treatment is effective in inhibiting viremia. 
1. Bordier BB, Ohkanda J, Liu P et al. In vivo antiviral efficacy of prenylation inhibitors against hepatitis delta virus. J Clin Invest. 2003 Aug;112(3):407-14.
2. Lerner EC, Qian Y, Blaskovich MA et al. Ras CAAX peptidomimetic FTI-277 selectively blocks
oncogenic Ras signaling by inducing cytoplasmic accumulation of inactive Ras-Raf complexes. J Biol Chem. 1995 Nov 10;270(45):26802-6. PubMed PMID: 7592920.