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You are here:Home-Inhibitors & Agonists-Metabolic Enzyme/Protease-Farnesyl transferase (FTase)

Request The Product List ofFarnesyl transferase (FTase) Farnesyl transferase (FTase)

Farnesyltransferase is one of the three enzymes in the prenyltransferase group. Farnesyltransferase's targets include members of the Ras superfamily of small GTP-binding proteins critical to cell cycle progression.

Farnesyltransferase inhibitors (FTIs) are small-molecule inhibitors that selectively inhibit farnesylation of a number of intracellular substrate proteins such as Ras. Farnesyl transferase inhibitors (FTIs) represent a new class of signaling inhibitors that is emerging in the clinical arena of hematologic malignancies and that may inhibit critical growth and survival signals. FTIs are a class of experimental cancer drugs that target protein farnesyltransferase with the downstream effect of preventing the proper functioning of the Ras (protein), which is commonly abnormally active in cancer.

Cat. No. Product Name CAS No. Information
H5137

FTI-277

 		170006-73-2

A peptide mimetic of the C-terminal Cys-Val-Ile-Met of K-Ras4B that potently inhibits FTase (Farnesyltransferase) with IC50 of 0.5 nM; highly selective for FTase over GGTase I (IC50 = 50 nM); extremely potent (IC50=100 nM) at inhibiting H-Ras in whole cells; blocks Ras oncogenic signaling by accumulating inactive Ras/Raf complexes in the cytoplasm.
H5136

ABT-100

 		450839-40-4

ABT-100 (ABT100) is a highly selective, potent, orally bioavailable inhibitor of farnesyltransferase (FTase); inhibits proliferation of cells in vitro carrying oncogenic H-Ras (EJ-1 bladder, IC50=2.2 nM), K-Ras (DLD-1 colon, MDA-MB-231 breast, HCT-116 colon, and MiaPaCa-2 pancreatic, IC50=3.8-9.2 nM), and wild-type Ras (PC-3 and DU-145, IC50=70 and 818 nM); inhibits in vivo growth of a series of xenografts.
H5141

Tipifarnib S enantiomer

 		192185-71-0

Tipifarnib S enantiomer is a potent and selective inhibitor of FTase (farnesyltransferase); inhibits the farnesylation of lamin B and K-RasB peptide substrates with IC50s of 0.86 nM and 7.9 nM, respectively; no activity for PGGT1(IC50>50 uM); shows sensiticity for tumor cell lines bearing H-ras or N-ras mutations; inhibits the growth of tumors bearing mice and orally bioavailable.
H5140

Tipifarnib

 		192185-72-1

Tipifarnib ((IND 58359, R115777)?is a potent and selective inhibitor of FTase (farnesyltransferase); inhibits the farnesylation of lamin B and K-RasB peptide substrates with IC50s of 0.86 nM and 7.9 nM, respectively; no activity for PGGT1(IC50>50 uM); shows sensiticity for tumor cell lines bearing H-ras or N-ras mutations; inhibits the growth of tumors bearing mice and orally bioavailable.
H5139

LB42908

 		226927-89-5

LB42908 is a highly potent, selective, orally active inhibitor of Ras farnesyltransferase (FTase) with IC50 of 0.9 nM against H-Ras and 2.4 nM against K-Ras.
H5138

FTI-277 hydrochloride

 		180977-34-8

A peptide mimetic of the C-terminal Cys-Val-Ile-Met of K-Ras4B that potently inhibits FTase (Farnesyltransferase) with IC50 of 0.5 nM; highly selective for FTase over GGTase I (IC50 = 50 nM); extremely potent (IC50=100 nM) at inhibiting H-Ras in whole cells; blocks Ras oncogenic signaling by accumulating inactive Ras/Raf complexes in the cytoplasm.

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