farnesyl

Farnesyl Pyrophosphate ammonium (Farnesyl diphosphate ammonium) is a metabolic intermediate of the MVA pathway that acts as a newly identified danger signal to trigger acute cell death and induce neuronal loss in stroke.

S-Farnesyl thioacetic acid, an analog of S-farnesyl cysteine, acts as a competitive inhibitor of isoprenylated protein methyltransferase (S-adenosylmethionine-dependent methyltransferase) and inhibits the methylation of both farnesylated and geranylgeranylated substrates.

Farnesyl acetate (Farnesyl Acetate (mixture of isomers)) is a flavouring compound identified in foods such as blueberries.

Farnesylacetone ((5E,9E)-6,10,14-Trimethylpentadeca-5,9,13-trien-2-one) is a marine derived natural products found in Sargassum micracanthum.

Farnesyl Pyrophosphate ammonium salt is an isomer of (E,E)-Farnesyl Pyrophosphate ammonium salt, which is a key metabolic intermediate in the mevalonate (MVA) pathway and an agonist of TRPM2, and is involved in cholesterol synthesis, ubiquinone synthesis, protein farnesylation and other physiological processes.

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.

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

BPH-1358 (NSC-50460) (NSC-50460) is a potent human farnesyl diphosphate synthase (FPPS) and undecaprenyl diphosphate synthase (UPPS) inhibitor. With IC50s of 1.8 μM and 110 nM, respectively. And it is active against S. aureus in vitro (MIC ~250 ng/mL)[1][2].

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

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

Risedronic Acid (Risedronate), a pyridinyl biphosphonate, can inhibit osteoclast-mediated bone resorption.

Risedronate Sodium (NE 58095 Sodium) is an aminobisphosphonate derivative of etidronic acid and CALCIUM CHANNEL BLOCKER that inhibits BONE RESORPTION and is used for the treatment of OSTEOPOROSIS.

Salirasib (Farnesyl Thiosalicylic Acid)(Ki=2.6 μM), an effective competitive prenylated protein methyltransferase (PPMTase) inhibitor, inhibits Ras methylation with potential antineoplastic activity.

Alendronate sodium hydrate (MK 217) is a nitrogen-containing bisphosphonate, which is an effective inhibitor of bone resorption. It is utilized for the treatment and prevention of osteoporosis.

Minodronic acid monohydrate is an farnesyl diphosphate synthase inhibitor that acts as a bone resorption inhibitor.

Arazine (N-Acetyl-S-farnesyl-L-cysteine) is a cell-permeable modulator of G protein and GPCR signaling, and it can act as a substrate for isoprenylcysteine methyltransferase by competing with prenylated G protein or its receptor sites.

BPH-1358 (NSC50460) free base is a potent human undecaprenyl diphosphate synthase (UPPS) and farnesyl diphosphate synthase (FPPS) inhibitor (IC50s: 110 nM and 1.8 μM) and is active against S. aureus in vitro (MIC ~250 ng/mL).

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.

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.

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.

Farnesyl pyrophosphate-d2 (Farnesyl diphosphate-d2) triammonium is the deuterium-labeled version of Farnesyl pyrophosphate triammonium. This compound, also known as Farnesyl pyrophosphate ammonium salt, is a 15-carbon isoprenoid and a metabolic intermediate in the mevalonate (MVA) pathway. It acts as an agonist of TRPM2 (TRP Channel), enabling the channel to open and allowing ion flow into cells. Additionally, Farnesyl pyrophosphate ammonium salt serves as a crucial branching substrate for cholesterol synthesis, ubiquinone synthesis, protein prenylation, and the synthesis of geranylgeranyl pyrophosphate (GGPP).