2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. Farnesyl Transferase

Farnesyl Transferase

Ftase

Farnesyl Transferase

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Farnesyl transferase is a zinc-dependent enzyme that catalyzes the attachment of a farnesyl lipid group to the sulfur atom of a cysteine residue of numerous proteins involved in cell signaling including the oncogenic H-Ras protein. Farnesyl transferase regulates the activation of Ras protein and consequently affects intracellular signal transduction, cell growth and proliferation.

Farnesyl transferase is an essential enzyme at downstream of mevalonate (MVA) pathway. Farnesyl transferase catalyzes the farnesylmoieties of farnesyl pyrophosphate (FPP) coupled to Ras protein, which is dependent on farnesylation anchoring itself in membrane for its activity. Farnesyl transferase inhibitors are small-molecule inhibitors that selectively inhibit farnesylation of a number of intracellular substrate proteins such as Ras. Farnesyl transferase inhibitors represent a new class of agents that target signal transduction pathways responsible for the proliferation and survival of diverse malignant cell types.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-10502
    Tipifarnib
    		Inhibitor 99.89%
    Tipifarnib (IND 58359) binds to and inhibits farnesyltransferase (FTase) with an IC50 of 0.86 nM. Antineoplastic activity and antiparasitic activity.
    Tipifarnib
  • HY-15136
    Lonafarnib
    		Inhibitor 99.85%
    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.
    Lonafarnib
  • HY-11101
    Alendronate sodium hydrate
    		Inhibitor 98.0%
    Alendronate (sodium hydrate) is a farnesyl diphosphate synthase inhibitor with IC50 of 460 nM.
    Alendronate sodium hydrate
  • HY-16273
    L-778123
    		99.92%
    L-778123 is a dual FPTase and GGPTase-I inhibitor, with IC50s of 2 nM and 98 nM respectively.
    L-778123
  • HY-16273A
    L-778123 hydrochloride
    		Inhibitor 99.85%
    L-778123 hydrochloride is a dual inhibitor of FPTase and GGPTase-I, with IC50 values of 2 nM and 98 nM respectively.
    L-778123 hydrochloride
  • HY-126472
    BPH252
    		Inhibitor
    BPH252 (Compound 4) is a geranylgeranyl diphosphate synthase inhibitor. BPH252 can be used in research on bisphosphonate-based anticancer inhibitors.
    BPH252
  • HY-117893
    BIM-46068
    		Inhibitor
    BIM-46068 is a potent, selectively human brain Farnesyltransferase (FTase) inhibitor (IC50 = 91.4 nM). BIM-46068 can specifically inhibit Ras processing in MiaPaCa-2 cancer cells. BIM-46068 can be used for the study of pancreatic cancer.
    BIM-46068
  • HY-116595
    J-104118
    		Inhibitor
    J-104118 is a potent and orally active squalene synthase (SQS) inhibitor with an IC50 of 0.52 nM. J-104118 inhibits cholesterol synthesis in mice. J-104118 can be used for cholesterol-lowering research.
    J-104118
  • HY-N6796
    Manumycin A
    		Inhibitor 99.27%
    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.
    Manumycin A
  • HY-15872A
    FTI-277 hydrochloride
    		Inhibitor 98.29%
    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.
    FTI-277 hydrochloride
  • HY-100313A
    YM-53601
    		Inhibitor 99.37%
    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.
    YM-53601
  • HY-16111
    BMS-214662
    		Inhibitor 99.86%
    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.
    BMS-214662
  • HY-128350
    FGTI-2734
    		Inhibitor 99.85%
    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.
    FGTI-2734
  • HY-16059
    Arglabin
    		Inhibitor 99.87%
    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.
    Arglabin
  • HY-16011
    NE 10790
    		Inhibitor 99.50%
    NE 10790, a poor farnesyl pyrophosphate synthase inhibitor, is a phosphonocarboxylate analogue of the potent bisphosphonate risedronate and is a weak antiresorptive agent.
    NE 10790
  • HY-16274
    Lapaquistat acetate
    		Inhibitor 99.10%
    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.
    Lapaquistat acetate
  • HY-16322
    Minodronic acid
    		Inhibitor 99.67%
    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.
    Minodronic acid
  • HY-16373
    CP-609754
    		Inhibitor 99.49%
    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.
    CP-609754
  • HY-123242
    FTI-2153
    		Inhibitor 99.77%
    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.
    FTI-2153
  • HY-116514
    (S)-(−)-Perillyl alcohol
    		Inhibitor 98.0%
    (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.
    (S)-(−)-Perillyl alcohol
Cat. No. Product Name / Synonyms Application Reactivity