farnesyl transferase (ftase)

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

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.

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

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

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).

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.

α-hydroxy Farnesyl phosphonic acid, a nonhydrolyzable analog of farnesyl pyrophosphate, acts as a competitive inhibitor of farnesyl transferase (FTase). At concentrations above 1 μM, it inhibits the processing of Ras in Ha-ras-transformed NIH3T3 cells.

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-IN-1 (compound 17a) is a highly effective farnesyl transferase (FTase) inhibitor with an IC50 value of 0.35 μM, demonstrating significant cytotoxicity and potent antitumor activity [1].

Tubulin polymerization-IN-25 is a selective, dual tubulin polymerization (IC50: 1.11 μM) and farnesyl transferase (FTase) (IC50: 0.39 μM) inhibitor. polymerization-IN-25 exhibits cytotoxicity against cancer cells and blocks cell proliferation.

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.

GGTI-297 is a potent, cell-permeable, and selective peptidomimetic inhibitor of GGTase I compared to Farnesyl Transferase (FTase).

(Rac)-Lonafarnib (Sch66336 racemate) is the racemic form of the potent, orally active farnesyl transferase (FTase) inhibitor, Lonafarnib. It effectively inhibits H-ras, K-ras, and N-ras with IC50 values of 1.9 nM, 5.2 nM, and 2.8 nM, respectively, and exhibits activities against the hepatitis delta virus (HDV).

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