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-163452
    Squalene synthase-IN-2
    		Inhibitor
    Squalene synthase-IN-2 (comppund isomer A-(1S, 3R)-14i) is an orally active squalene synthase inhibitor with IC50 values of 3.4, 99 nM for squalene synthase and cholesterol synthesis, respectively. Squalene synthase-IN-2 reduces plasma cholesterol and triglyceride.
    Squalene synthase-IN-2
  • HY-15136B
    (Rac)-Lonafarnib
    (Rac)-Lonafarnib (Sch66336 racemate) is the racemate of Lonafarnib. Lonafarnib 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.
    (Rac)-Lonafarnib
  • HY-118916
    FTI-2148
    		Inhibitor
    FTI-2148 is a RAS C-terminal mimetic dual farnesyl transferase (FT-1) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC50s of 1.4 nM and 1.7 μM, respectively.
    FTI-2148
  • HY-100299
    RPR107393 free base
    		Inhibitor
    RPR107393 free base is an orally active potent selective squalene synthase (SQS) inhibitor. RPR107393 free base inhibits rat liver microsomal squalene synthase with an IC50 value of 0.8 nM. RPR107393 free base reduces triglyceride biosynthesis by suppressing fatty acid biosynthesis via an increase in intracellular farnesol and its derivatives. RPR107393 free base reduces plasma cholesterol in rats and marmosets. RPR107393 free base can be used for metabolic disease research, such as hypercholesterolemia, hypertriglyceridemia and atherosclerosis[1][2].
    RPR107393 free base
  • HY-16108A
    BMS-187745 tripotassium
    		Inhibitor
    BMS-187745 tripotassium (Compound 1) is a potent squalene synthase inhibitor.
    BMS-187745 tripotassium
  • HY-N3378
    Lipiferolide
    		Inhibitor
    Lipiferolide is an antiplasmodial agent (IC50: 1.8 μg/mL) that can be isolated from Liriodendron tulipifera. Lipiferolide also inhibits FPTase, and has antitumor activity.
    Lipiferolide
  • 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-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-116428
    L-744832
    		Inhibitor
    L-744832 is a farnesyl transferase inhibitor. L-744832 effectively inhibits the farnesylation of H-Ras and N-Ras, but has little effect on K-Ras treatment. L-744832 not only directly targets the oncogenic pathway by inhibiting Ras farnesylation, but also enhances radiosensitivity by restoring TGF-β signaling through epigenetic reprogramming. L-744832 can induce cell cycle arrest and apoptosis. L-744832 can be used in combination therapy studies for Ras-driven tumors such as pancreatic cancer.
    L-744832
  • 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-178158
    SQS-IN-1
    		Inhibitor
    SQS-IN-1 is a squalene synthase (SQS) inhibitor. SQS-IN-1 exhibits potent and broad-spectrum anti-proliferative effects on both mouse and human lung cancer cell lines. SQS-IN-1 inhibits DNA replication and the cell cycle, causing mitochondrial hyperpolarization and inducing cell apoptosis. SQS-IN-1 inhibits cell migration and invasion. SQS-IN-1 can be used to the study of lung cancer.
    SQS-IN-1
  • 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-10062
    AZD3409
    		Inhibitor
    AZD3409 is a prenyl inhibitor that exhibits inhibitory activity against both farnesyl transferase and geranylgeranyl transferase I. AZD3409 inhibits the growth of breast cancer cells, with IC50s of 220 nM (MDA-MB-468), 180 nM (MDA-MB-361), and 290 nM (SK-Br-3). AZD3409 significantly reduces the activation level of AKT in breast cancer cell lines. AZD3409 induces G0/G1 phase arrest in MDA-MB-468 cells, causes G2/M phase arrest in MDA-MB-361 cells. AZD3409 can be used for the study of breast cancer.
    AZD3409
  • 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.
    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
Cat. No. Product Name / Synonyms Application Reactivity