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-N13876
    Andrastin D
    		Inhibitor
    Andrastin D is a protein farnesyltransferase inhibitor. Andrastin D has a common androstane skeleton.
    Andrastin D
  • HY-124723
    Gerfelin
    		Inhibitor
    Gerfelin inhibits geranylgeranyl diphosphate synthase (GGPP synthase) activity with an IC50 of 3.5 μg/mL.
    Gerfelin
  • HY-110038
    FTI-277 TFA
    		Inhibitor
    FTI-277 TFA is a farnesyltransferase (FTase) inhibitor. FTI-277 TFA inhibits Ras farnesylation, blocks the phosphorylation of downstream ERK1/2 and mTOR, and reduces membrane-bound active N-ras protein. FTI-277 TFA activates caspase 3, upregulates Bim expression, induces cell apoptosis, suppresses regulatory T cell expansion, enhances macrophage phagocytosis, and improves bacterial clearance. FTI-277 TFA activates the PI3K/Akt signaling pathway, inhibits osteoblast differentiation, and reduces the proliferation ability of neuroblastoma cells. FTI-277 TFA can be used in research related to head and neck squamous cell carcinoma, neuroblastoma, sepsis, and vascular calcification.
    FTI-277 TFA
  • HY-120614
    BMS-186511
    		Inhibitor
    BMS-186511 is a farnesyltransferase (FT) inhibitor and shows anticancer activity.
    BMS-186511
  • HY-122469
    Kurasoin B
    		Inhibitor
    Kurasoin B is a protein farnesyltransferase inhibitor (IC50: 58.7 μM). Kurasoin B can be produced by Paecilomyces sp. FO-3684.
    Kurasoin B
  • HY-126871
    Zaragozic acid D2
    		Inhibitor
    Zaragozic acid D2 is the inhibitor for squalene synthase and Ras farnesyl-protein transferase (Ras FPTase), with IC50 of 2 nM and 100 nM, respectively. Zaragozic acid D2 is potentially ameliorating hypercholesterolemia and Ras-induced cancer.
    Zaragozic acid D2
  • HY-137139
    10'-Desmethoxystreptonigrin
    		Inhibitor
    10'-Desmethoxystreptonigrin is an inhibitor for Ras Farnesyltransferase with an IC50 of 21 μM. 10'-Desmethoxystreptonigrin is a broad-spectrum antibiotic with antibacterial activity. 10'-Desmethoxystreptonigrin exhibits antitumor activity against P388 leukemia, without significant cytotoxicity (LD50 is 8.8 mg/kg).
    10'-Desmethoxystreptonigrin
  • HY-182516
    Aminobutane bisphosphonate
    		Inhibitor
    Aminobutane bisphosphonate is a Trypanosoma cruzi farnesyl pyrophosphate synthase (FPPS) inhibitor with an IC50 of 30.77 μM against Trypanosoma cruzi. Aminobutane bisphosphonate inhibits proliferation of intracellular amastigote Trypanosoma cruzi and lacks activity against non-infective epimastigote forms. Aminobutane bisphosphonate reduces osteoclastic bone resorption, osteoid surface extent, and osteoclast number per mm of bone surface. Aminobutane bisphosphonate can be used for the research of american trypanosomiasis (chagas' disease) and immobilization-related bone loss.
    Aminobutane bisphosphonate
  • HY-U00327
    Prenyl-IN-1
    		Inhibitor
    Prenyl-IN-1 is a protein prenylation inhibitor, especially a geranylgeranyltransferase (GGT) or a farnesyltransferase (FT) inhibitor, exhibiting potent activity against oxidative stress, and particularly in the treatment of Parkinson's Disease.
    Prenyl-IN-1
  • HY-U00401
    (Rac)-CP-609754
    		Inhibitor
    (Rac)-CP-609754 is the racemate of CP-609754. CP-609754 is a farnesyltransferase inhibitor, used for the treatment of cancer and Alzheimer's disease.
    (Rac)-CP-609754
Cat. No. Product Name / Synonyms Application Reactivity