FTase Inhibitor II (trifluoroacetate salt) (Synonyms: Farnesyltransferase Inhibitor II, FTI-II) |
Catalog No.GC52503 |
A potent, selective inhibitor of farnesyltransferase
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
Farnesylation involves the utilization of farnesyl pyrophosphate (FPP), an intermediate in the mevalonate pathway, by farnesyltransferase (FTase) to add a lipid, farnesyl, to certain proteins.1,2 This post-translational modification is crucial in allowing target proteins, including Ras, to associate with, and function at, membranes. FTase Inhibitor II is a cell-permeable analog of FPP that potently inhibits FTase (IC50 = 50-75 nM), preventing farnesylation of Ras.3 It does not inhibit geranylgeranyl transferase at similar concentrations (IC50 > 100 µM).3 FTase Inhibitor II displays no toxicity to untransformed cells but blocks Ras-mediated transformation of NIH 3T3 cells.3
1.Berndt, N., Hamilton, A.D., and Sebti, S.M.Targeting protein prenylation for cancer therapyNat. Rev. Cancer11(11)775-791(2011) 2.Appels, N.M.G.M., Beijnen, J.H., and Schellens, J.H.M.Development of farnesyl transferase inhibitors: A reviewOncologist10(8)565-578(2005) 3.Manne, V., Ricca, C.S., Brown, J.G., et al.Ras farnesylation as a target for novel antitumor agents: Potent and selective farnesyl diphosphate analog inhibitors of farnesyltransferaseDrug Dev. Res.34(2)121-137(1995)
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