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-N7634
    Tectol
    		Inhibitor 99.72%
    Tectol, isolated from Lippia sidoides, exhibits significant activity against human leukemia cell lines HL60 and CEM. Tectol is a farnesyltransferase (FTase) inhibitor with IC50s of 2.09 and 1.73 μM for human and T. brucei FTase, respectively. Tectol inhibits drug-resistant strain of P. falciparum (FcB1) with an IC50 of 3.44 μM.
    Tectol
  • HY-128041
    alpha-Hydroxy farnesyl phosphonic acid
    		Inhibitor
    α-hydroxy Farnesyl phosphonic acid is a nonhydrolyzable analog of farnesyl pyrophosphate which acts as a competitive inhibitor of farnesyl transferase (FTase). At concentrations greater than 1 μM, α-hydroxy farnesyl phosphonic acid inhibits the processing of Ras in Ha-ras-transformed NIH3T3 cells.
    alpha-Hydroxy farnesyl phosphonic acid
  • HY-116290A
    Zaragozic acid A trisodium
    Zaragozic acid A trisodium is a fungal metabolite that acts as a reversible competitive inhibitor of squalene synthase.
    Zaragozic acid A trisodium
  • HY-125311
    Zaragozic acid D
    		Inhibitor
    Zaragozic acid D is a squalene synthase inhibitor. Zaragozic acid D also is a farnesyl-protein transferase (FPTase) inhibitor with an IC50 value of 100 nM for bovine FPTase.
    Zaragozic acid D
  • HY-16111A1
    BMS-214662 mesylate
    		Inhibitor
    BMS-214662 mesylate is a potent and selective farnesyl transferase inhibitor with an IC50 of 1.35 nM. BMS-214662 mesylate exhibits potent antitumor activity and can be utilized in cancer research.
    BMS-214662 mesylate
  • HY-117807
    A-176120
    		Inhibitor
    A-176120 is a selective inhibitor of farnesyl transferase (IC50=1.2 nM) based on a farnesyl pyrophosphate (FPP) analog, with superior selectivity against GGTaseI (IC50=423 nM), GGTaseII (IC50=3000 nM), and SSase (IC50>10 μM). A-176120 inhibits ras processing in H-ras transformed NIH3T3 cells and HCT116 K-ras mutant cells (ED50=1.6 and 0.5 μM, respectively). A-176120 has antiangiogenic and antitumor activities in vivo and reduces capillary structure formation and VEGF secretion.
    A-176120
  • HY-124205
    Pepticinnamin E
    		Inhibitor
    Pepticinnamin E is a Farnesyltransferase (FTase) inhibitor (IC50=42 µM). Pepticinnamin E can be used in cancer and malaria research.
    Pepticinnamin E
  • HY-129273
    L-731735
    		Inhibitor
    L-731735 is a selective FPTase inhibitor that can inhibit ras-dependent cell transformation. L-731735 can be used in cancer research.
    L-731735
  • HY-151566
    Antifungal agent 46
    		Inhibitor
    Antifungal agent 46 (compound 2f) is a potent antifungal agent. Antifungal agent 46 prevents Ras signaling by inhibiting protein farnesyltransferase.
    Antifungal agent 46
  • HY-142655
    Ftase inhibitor III
    		Inhibitor
    Ftase inhibitor III is an anion-dependent Farnesyltransferase inhibitor from a phenotypic screen.
    Ftase inhibitor III
  • HY-100313
    YM-53601 free base
    		Inhibitor
    YM-53601 free base, a squalene synthase inhibitor, reduces plasma cholesterol and triglyceride levels in vivo. YM-53601 free base inhibits squalene synthase derived from human hepatoma cells with an IC50 of 79 nM. Lipid-lowering agent. YM-53601 free base is also an inhibitor of farnesyl-diphosphate farnesyltransferase 1 (FDFT1) enzyme activity and abrogates HCV propagation.
    YM-53601 free base
  • HY-100299A
    RPR107393
    		Inhibitor
    RPR107393 is an orally active potent selective squalene synthase (SQS) inhibitor. RPR107393 inhibits rat liver microsomal squalene synthase with an IC50 value of 0.8 nM. RPR107393 reduces triglyceride biosynthesis by suppressing fatty acid biosynthesis via an increase in intracellular farnesol and its derivatives. RPR107393 reduces plasma cholesterol in rats and marmosets. RPR107393 can be used for metabolic disease research, such as hypercholesterolemia, hypertriglyceridemia and atherosclerosis[1][2].
    RPR107393
  • HY-118426
    (Rac)-Tipifarnib
    		Inhibitor
    (Rac)-Tipifarnib ((Rac)-IND 58359; (Rac)-R115777) is a potent farnesyl protein transferase inhibitor that specifically targets the pro-tailation process of Ras proteins. (Rac)-Tipifarnib showed significant in vivo antitumor effects after oral administration to mice.
    (Rac)-Tipifarnib
  • 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-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
Cat. No. Product Name / Synonyms Application Reactivity