farnesyl transferase

BMS-214662 is a selective farnesyl transferase inhibitor with antitumor activity, useful in studies of pancreatic, head and neck, and lung cancers.

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

FGTI-2734 is a dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT-1) inhibitor, exhibiting IC50 values of 250 nM and 520 nM for FT and GGT-1, respectively. It effectively prevents the membrane localization of KRAS, addressing the issue of KRAS resistance and inhibiting the growth of mutant KRAS patient-derived pancreatic tumors.

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

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.

Tipifarnib (IND 58359) is a nonpeptidomimetic quinolinone with potential antineoplastic activity. Tipifarnib binds to and inhibits the enzyme farnesyl protein transferase, an enzyme involved in protein processing (farnesylation) for signal transduction. By inhibiting the farnesylation of proteins, this agent prevents the activation of Ras oncogenes, inhibits cell growth, induces apoptosis, and inhibits angiogenesis.

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

Arglabin ((+)-Arglabin) is a natural product isolated from Artemisia glabella, is a NLRP3 inflammasome inhibitor, has anti-atherogenic and anticancer effects.

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.

ABT-100 is a potent, highly selective, and orally active inhibitor of farnesyl transferase [farnesyl-protein transferase] with broad-spectrum antitumor activity.

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.

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

Perillyl Alcohol is a naturally occurring monoterpene related to limonene with antineoplastic activity. Perillyl alcohol (Isocarveol) inhibits farnesyl transferase and geranylgeranyl transferase, thereby preventing post-translational protein farnesylation and isoprenylation and activation of oncoproteins such as p21-ras, and arresting tumor cells in the G1 phase of the cell cycle.

The L-778123 hydrochloride is an inhibitor of FPTase (IC50: 2 nM) and GGPTase-I (IC50: 98 nM) in enzyme inhibition determination.

FGTI-2734 mesylate, a RAS C-terminal mimetic compound with dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT) inhibitory activities (IC50s of 250 nM and 520 nM for FT and GGT, respectively), mitigates KRAS resistance by preventing its membrane localization, effectively impeding mutant KRAS patient-derived pancreatic tumors.

FTI-2148 diTFA, a dual inhibitor targeting both farnesyl transferase (FT-1) and geranylgeranyl transferase-1 (GGT-1), functions as a RAS C-terminal mimetic. It exhibits potent inhibitory capabilities with IC50 values of 1.4 nM for FT-1 and 1.7 μM for GGT-1, respectively.

FTI-2148 is an inhibitor of RAS C-terminal mimetic dual farnesyl transferase (FT-1) and geranylgeranyl transferase-1 (GGT-1) (IC50s: 1.4 nM and 1.7 μM, respectively).

BMS-214662 mesylate is a potent and selective farnesyl transferase inhibitor with an IC50 of 1.35 nM. It exhibits antitumor activity and is applicable in cancer research.

Darlifarnib (Compound (S)-058) is an inhibitor of farnesyl transferase and geranylgeranyltransferase, with IC50 values of ≤ 10 nM and > 1000 nM, respectively. It exhibits high metabolic stability in human and mouse liver microsomes, with a half-life of over 100 minutes.

L 739749 is a CAAX peptidomimetic. It is also an inhibitor of farnesyl-protein transferase.

R 115777 is an inhibitor of farnesyl transferase.

Zaragozic acid D inhibits squalene synthase and ras farnesyl-protein transferase isolated from the keratinophilic fungus Amauroascus niger.

Zaragozic acid D(2) inhibits squalene synthase and ras farnesyl-protein transferase isolated from the keratinophilic fungus Amauroascus niger.