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

Farnesyl Transferase

Ftase

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-128044
    Ftase inhibitor I
    Inhibitor
    Ftase inhibitor I (B581) is a potent, selective and peptidomimetic farnesyl transferase (FTase) inhibitor. Ftase inhibitor I shows selectivity for FTase over geranylgeranyl isoprenoid (Ras-GG) or the fatty acid myristate (Myr-Ras).
    Ftase inhibitor I
  • HY-11101R
    Alendronate sodium hydrate (Standard)
    Inhibitor
    Alendronate (sodium hydrate) (Standard) is the analytical standard of Alendronate (sodium hydrate). This product is intended for research and analytical applications. Alendronate (sodium hydrate) is a farnesyl diphosphate synthase inhibitor with IC50 of 460 nM.
    Alendronate sodium hydrate (Standard)
  • HY-163832
    FPPS-IN-2
    Inhibitor
    FPPS-IN-2 (compound 4a) is a potent and orally active HFPPS inhibitor with an IC50 value of 1.108 µM. FPPS-IN-2 has the potential for the research of osteoporosis.
    FPPS-IN-2
  • HY-124374
    J-104123
    Inhibitor
    J-104123 is an inhibitor of squalene synthase with monocarboxylic acid structure. J-104123 can lower serum cholesterol level in dog models.
    J-104123
  • HY-129279
    Andrastin A
    Inhibitor
    Andrastin A meroterpenoid compound, is a farnesyltransferase inhibitor. Andrastin A inhibits the efflux of anticancer compounds from multidrug-resistant cancer cells. Andrastin A can be isolated from Penicillium species.
    Andrastin A
  • HY-B2097
    Incadronate disodium
    Inhibitor
    Incadronate disodium (YM 175) is a bisphosphonate with strong inhibitory activity on bone resorption. Incadronate disodium indirectly stimulates renal 25-hydroxyvitamin D-1-hydroxylase by increasing circulating parathyroid hormone. Incadronate disodium, a cholesterol-lowering agent, is a potent inhibitor of rat liver microsomal squalene synthase (Ki=57 nM). Incadronate disodium inhibits sterol biosynthesis in mouse macrophage J774 cells (IC50=64 μM). Incadronate disodium has the potential for malignant tumors research.
    Incadronate disodium
  • HY-123404
    L-731128
    Inhibitor
    L-731128 is a novel alkyl citrate. L-731128 can be isolated as a minor component of Sporormiella intermedia (MF 5447, ATCC 20985) fermentations. L-731128 is a potent squalene synthase inhibitor, with an IC50 value of 767 nM.
    L-731128
  • HY-N14820
    Kurasoin A
    Inhibitor
    Kurasoin A is a farnesyltransferase inhibitor.
    Kurasoin A
  • HY-N13874
    Andrastin B
    Inhibitor
    Andrastin C is a protein farnesyltransferase inhibitor. Andrastin C has a common androstane skeleton.
    Andrastin B
  • HY-N13888
    Schizostatin
    Inhibitor
    Schizostatin is a squalene synthase inhibitor with an IC50 of 0.84 μM.
    Schizostatin
  • HY-15136R
    Lonafarnib (Standard)
    Inhibitor
    Lonafarnib (Standard) is the analytical standard of Lonafarnib. This product is intended for research and analytical applications. Lonafarnib (Sch66336) is a potent and orally active 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 (Standard)
  • HY-120044
    L-739749
    Inhibitor
    L-739749 is a farnesyl transferase inhibitor. L-739749 inhibits the selective hypersensitivity of JMML cells to granulocyte-macrophage colony-stimulating factor (GM-CSF) by blocking the prenylation of Ras. L-739749 exhibits a strong inhibitory effect on the growth of primary human JMML cells in vitro.
    L-739749
  • HY-100313AR
    YM-53601 (Standard)
    Inhibitor
    YM-53601 (Standard) is the analytical standard of YM-53601 (HY-100313A). This product is intended for research and analytical applications. 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 (Standard)
  • HY-10502R
    Tipifarnib (Standard)
    Inhibitor
    Tipifarnib (Standard) is the analytical standard of Tipifarnib (HY-10502). This product is intended for research and analytical applications. Tipifarnib (IND 58359) binds to and inhibits farnesyltransferase (FTase) with an IC50 of 0.86 nM. Antineoplastic activity and antiparasitic activity.
    Tipifarnib (Standard)
  • HY-19301
    J 104871
    Inhibitor
    J 104871 (J-104135) is a farnesyl pyrophosphate (FPP)-competitive farnesyltransferase (FTase) inhibitor. J 104871 inhibits rat brain FTase with an IC50 of 3.9 nM in the presence of farnesyl pyrophosphate (FPP).
    J 104871
  • HY-N9604
    Andrastin C
    Inhibitor
    Andrastin B is a protein farnesyltransferase inhibitor. Andrastin B has a common androstane skeleton.
    Andrastin C
  • HY-125669
    XR 3054
    Inhibitor
    XR 3054 is an inhibitor for Farnesyl Transferase, that inhibits farnesylation of CAAX recognition peptide with IC50 of 50 μM. XR 3054 suppresses the farnesylation of p21 ras and activation of MAP kinase. XR 3054 inhibits the proliferation of prostate cancer cell and colon cancer cell, with IC50 of 8.8-21.4 μM.
    XR 3054
  • HY-16273B
    L-778123 dihydrochloride
    Inhibitor
    L-778123 dihydrochloride is a dual FPTase and GGPTase-I inhibitor, with IC50s of 2 nM and 98 nM, respectively.
    L-778123 dihydrochloride
  • HY-134579
    Chaetomellic acid A
    Inhibitor
    Chaetomellic acid A can be isolated from Chaetomella acutiseta. Chaetomellic acid A is a specific inhibitor of farnesyl-protein transferase. Chaetomellic acid A decreases oxidative stress-induced apoptosis in cells. Chaetomellic acid A reduces renal damage after unilateral ureteral obstruction (UUO) in mice.
    Chaetomellic acid A
  • HY-123746
    E5700
    Inhibitor
    E5700 is an orally active squalene synthase inhibitor, antimalarial agent and antifungal agent with an IC50 of 0.49 nM (without PPi) against squalene synthase from T. cruzi epimastigotes. E5700 shows antiparasitic activities against Trypanosoma cruzi. E5700 inhibits the growth and alters the lipid prolife and the ultrastructure of a multiple agent-resistant C. tropicalis strain. E5700 is a potent and selective inhibitor of the growth of Leishmania amazonensis.
    E5700
Cat. No. Product Name / Synonyms Application Reactivity