farnesyltransferase

Lonafarnib (Sch66336) is an orally bioavailable FPTase inhibitor for H-ras, K-ras-4B, and N-ras (IC50: 1.9 5.2 2.8 nM).

Tectol has anti-plasmodial activity, it as a moderately active growth inhibitor with an IC50 3.44±0.20μM. It exhibited significant activity against human leukemia cell lines HL60 and CEM. Tectol may cause itchy dermatitis, the dermatitis appeared on the n

Prenyl-IN-1 is a potent and selective prenylation inhibitor of geranylgeranyltransferase or farnesyltransferase.Prenyl-IN-1 shows anti-oxidative stress effects in a Parkinson's model. Prenyl-IN-1 showed anti-oxidative stress in a Parkinson's model.

J-104871 (UNII-6137X5QNJF) is a novel farnesyltransferase (FTase) inhibitor that competitively blocks Ras farnesylation in vivo, inhibits Ras processing in activated H-ras-transformed NIH3T3 cells, and suppresses tumor growth in nude mice transplanted with activated H-ras-transformed NIH3T3 cells.

A-176120 ammonium is a novel farnesyl pyrophosphate analog with antitumor and antiangiogenic properties and inhibits farnesyltransferase activity.

LB42708 is an orally active farnesyltransferase (FTase) inhibitor (IC50: 0.8 1.2 2.0 nM toward H N K-ras).

L-739,750 is an inhibitor (FTI) of peptidomimetic farnesyltransferase.

L-739750 2HCl is a potent inhibitor of peptidomimetic farnesyltransferase, a novel pseudopeptide mimetic with potential anticancer activity.

A-176120 is a potent farnesyl pyrophosphate (FPP) analogues, it selectively inhibits farnesyltransferase. It has anti-angiogenic potential and may reduce H-ras NIH3T3 tumour growth.

FTI-277 hydrochloride (FTI 277 HCl) is an effective and specific farnesyltransferase (FTase) inhibitor (IC50: 500 pM); this selectivity is about 100-fold than the closely related GGTase I.

FTI-276 is an inhibitor of protein farnesyltransferase (PFT) (IC50s: 0.9 and 0.5 nM for Plasmodium falciparum and human).

FTI-2153 is a potent and highly selective farnesyltransferase (FTase) inhibitor (IC50: 1.4 nM) that is over 3000-fold more effective at blocking H-Ras (IC50: 10 nM) than Rap1A processing.

LNK754 is a farnesyltransferase inhibitor. It is used for the treatment of cancer and Alzheimer's disease.

Manumycin A is an antibiotic with anticancer activity and is a mammalian thioredoxin reductase-1 (TrxR-1) inhibitor.Manumycin A inhibits the production of IL-1β, IL-6, and IL-8 in TNF alpha-stimulated THP-1 cells and peripheral blood mononuclear cells in a dose-dependent manner, inducing apoptosis.

Tipifarnib S enantiomer ((S)-(-)-R-115777) is the S-enantiomer of Tipifarnib. Tipifarnib is a potent and specific farnesyltransferase inhibitor (IC50: 0.6 nM).

Andrastin B is an inhibitor of the protein farnesyltransferase. It possesses a typical androstan backbone.

Kurasoin B is an inhibitor of protein farnesyltransferase.

L 731734 is a farnesyltransferase inhibitor.

L 731735 is a farnesyltransferase inhibitor.

Pepticinnamin E is a naturally occurring bisubstrate farnesyltransferase inhibitor.

YM-53601 is a potent squalene synthase (SQS) inhibitor that inhibits adipogenic biosynthesis and lipid secretion in rodents.YM-53601 is a cholesterol-lowering agent that inhibits farnesyl diphosphate farnesyltransferase 1 (FDFT1).YM-53601 exhibits potential antiviral activity and enhances adriamycin-mediated HCC arrest and cell death in vivo. MJN228 is a lipid-based enzyme.

CP-609754 (LNK-754) is a potent and reversible farnesyltransferase inhibitor with potential anticancer activity. It inhibits farnesylation of recombinant human H-Ras (IC50=0.57 ng mL) and K-Ras (IC50=46 ng mL)[1]. In 3T3 H-ras (61L)-transfected cell lines, CP-609754 exhibits a slow on off rate, inhibiting mutant H-Ras farnesylation with an IC50 of 1.72 ng mL[1]. The compound is competitive for the prenyl acceptor (H-Ras protein) and noncompetitive for the prenyl donor farnesyl PPI, selectively inhibiting farnesylation of both H- and K-Ras proteins in 3T3 transfectants[1]. In vivo, CP-609754 shows antitumor activity against 3T3 H-ras (61L) tumors, with tumor regression achieved at 100 mg kg twice daily and an ED50 for tumor growth inhibition at 28 mg kg[1]. Continuous i.p. infusion of CP-609754 inhibits tumor growth by over 50% and reduces tumor farnesyltransferase activity by over 30% when plasma concentration is maintained above 118 ng mL[1]. [1]. Stacy L Moulder, et al. A phase I open label study of the farnesyltransferase inhibitor CP-609,754 in patients with advanced malignant tumors. Clin Cancer Res. 2004 Nov 1;10(21):7127-35.

Ftase Inhibitor III, derived from a phenotypic screen, functions as an anion-dependent inhibitor of Farnesyltransferase.

FTI 277 TFA is a prodrug form of FTI 276 that inhibits farnesyltransferase (FTase) (IC50 = 0.5 nM). Inhibits H-Ras and K-Ras processing in whole cells (IC50 values are 0.1 and 10μM respectively) and disrupts constitutive H-Ras-specific activation of MAPK. Causes significant antiproliferative effects in human malignant glioma cells and many other tumor cell lines.