Farnesyl Transferase Inhibitor

Tipifarnib (IND 58359) binds to and inhibits farnesyltransferase (FTase) with an IC₅₀ of 0.86 nM. Antineoplastic activity and antiparasitic activity.

Lonafarnib (Sch66336) is a potent and orally active, and CNS-penetrant farnesyl transferase (FTase) inhibitor. Lonafarnib inhibits the activities of H-ras, K-ras and N-ras with IC₅₀ values of 1.9 nM, 5.2 nM and 2.8 nM, respectively. Lonafarnib also has anti-hepatitis delta virus (HDV) activities.

Alendronate (sodium hydrate) is a farnesyl diphosphate synthase inhibitor with IC₅₀ of 460 nM.

L-778123 hydrochloride is a dual inhibitor of FPTase and GGPTase-I, with IC₅₀ values of 2 nM and 98 nM respectively.

BPH252 (Compound 4) is a geranylgeranyl diphosphate synthase inhibitor. BPH252 can be used in research on bisphosphonate-based anticancer inhibitors.

FTase-IN-2 (Compound 2) is a farnesyltransferase inhibitor, with IC₅₀ values of 150 nM and 1500 nM against FTase and GGTase I, respectively. FTase-IN-2 is not farnesylated by FTase, thus avoiding metabolic inactivation.

Manumycin A is a polyketide antibiotic and an inhibitor of thioredoxin reductase 1 (TrxR-1). Manumycin A can inhibit the growth of breast cancer cells and exert its anti-tumor activity through LC3. Manumycin A can downregulate the release of pro-inflammatory cytokines in human monocytes stimulated by TNF α, and has potential anti-inflammatory activity. Manumycin A can inhibit the Ras/Raf/ERK1/2 signaling and hnRNP H1 in castration resistant prostate cancer cells to suppress exosome biogenesis and secretion.

FTI-277 hydrochloride is an inhibitor of farnesyl transferase (FTase); a highly potent Ras CAAX peptidomimetic which antagonizes both H- and K-Ras oncogenic signaling. FTI-277 hydrochloride can inhibit hepatitis delta virus (HDV) infection.

YM-53601, a squalene synthase inhibitor, reduces plasma cholesterol and triglyceride levels in vivo. YM-53601 inhibits squalene synthase derived from human hepatoma cells with an IC₅₀ of 79 nM. Lipid-lowering agent. YM-53601 is also an inhibitor of farnesyl-diphosphate farnesyltransferase 1 (FDFT1) enzyme activity and abrogates HCV propagation.

FGTI-2734 is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC₅₀s of 250 nM and 520 nM for FT and GGT-1, respectively. FGTI-2734 can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors.

BMS-214662 is a farnesyl transferase inhibitor. BMS-214662 can effectively block the localization and function of Ras protein in the cell membrane by inhibiting the pro-group modification of Ras protein, thereby exerting anti-tumor activity. BMS-214662 has an IC₅₀ value of 1.3 nM for H-Ras and 8.4 nM for K-Ras. BMS-214662 can be used to study Ras-related tumor diseases.

NE 10790, a poor farnesyl pyrophosphate synthase inhibitor, is a phosphonocarboxylate analogue of the potent bisphosphonate risedronate and is a weak antiresorptive agent.

Arglabin ((+)-Arglabin), a natural product isolated from Artemisia glabella, is a NLRP3 inflammasome inhibitor. Arglabin shows anti-inflammatory and antitumor activities. The antitumor activity of Arglabin proceeds through its inhibition of farnesyl transferase which leads to the activation of RAS proto-oncogene.

Lapaquistat acetate (TAK-475) is a squalene synthase inhibitor, blocking the conversion of farnesyl diphosphate (FPP) to squalene in the cholesterol biosynthesis pathway. Lapaquistat acetate is effective at lowering low-density lipoprotein cholesterol, but it might cause liver damage. Lapaquistat acetate is used for hypercholesterolemia and mevalonate kinase deficiency (MKD) research.

(S)-(-)-Perillyl alcohol, a monoterpene, is an orally active farnesyl transferase and geranylgeranyl transferase inhibitor. (S)-(-)-Perillyl alcohol up-regulates the mannose-6-phosphate receptor, facilitating TGF-β1 activation and cytostasis,. (S)-(-)-Perillyl alcohol induces apoptosis in cancer cells, modulates cyclin D1 and AP-1 activity. (S)-(-)-Perillyl alcohol exhibits antitumor activity against sarcoma tumors in mice. (S)-(-)-Perillyl alcohol can be used for the research of squamous cell carcinoma of the esophagus and sarcoma 180.

Minodronic acid (YM-529) is an FPP synthase inhibitor with an IC₅₀ of 3 nM, and also an antagonist of P2X2/3 receptors with an IC₅₀ of 62.7 μM. Minodronic acid induces tumor cell apoptosis and inhibits cell growth. Minodronic acid also suppresses bone resorption. Minodronic acid can be used in research related to osteoporosis and cancer.

FTI-2153 is a potent and highly selective inhibitor of farnesyltransferase (FTase), with an IC₅₀ of 1.4 nM. FTI-2153 is >3000-fold more potent at blocking H-Ras (IC₅₀, 10 nM) than Rap1A processing. Anti-cancer activity.

CP-609754 (LNK-754) is a potent and reversible farnesyltransferase inhibitor with potential anticancer activity.The IC₅₀ for inhibiting farnesylation of recombinant human H-Ras is 0.57 ng/mL and recombinant K-Ras is 46 ng/mL. CP-609754 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

LB42708 is a potent, selective and orally active farnesyltransferase inhibitor. LB42708 inhibits farnesylation of H-Ras, N-Ras and K-Ras4B with IC₅₀s of 0.8 nM, 1.2 nM and 2.0 nM, respectively.

FGTI-2734 mesylate is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT) inhibitor with IC₅₀s of 250 nM and 520 nM for FT and GGT, respectively. FGTI-2734 mesylate can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors.