A cell-permeable analog of FPP that potently inhibits FTase (IC50 = 50-75 nM)

FTase Inhibitor II – 1 mg

Brand:
Cayman
CAS:
156707-43-6
Storage:
-20
UN-No:
Non-Hazardous - /

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.{26419,21707} 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.{27760} It does not inhibit geranylgeranyl transferase at similar concentrations (IC50 > 100 µM).{27760} FTase Inhibitor II displays no toxicity to untransformed cells but blocks Ras-mediated transformation of NIH 3T3 cells.{27760}  

 

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Description

A cell-permeable analog of FPP that potently inhibits FTase (IC50 = 50-75 nM), preventing farnesylation of Ras; does not inhibit geranylgeranyl transferase at similar concentrations (IC50 > 100 µM); blocks Ras-mediated transformation of NIH 3T3 cells

Formal name: N-[4-[[(2R)-2-amino-3-mercapto-1-oxopropyl]amino]benzoyl]-L-methionine

Synonyms:  Farnesyltransferase Inhibitor II|FTI-II

Molecular weight: 371.5

CAS: 156707-43-6

Purity: ≥80%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer|Cell Signaling|GTPases

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