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-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-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-110038
    FTI-277 TFA
    Inhibitor
    FTI-277 TFA is an inhibitor of farnesyl transferase (FTase); a highly potent Ras CAAX peptidomimetic which antagonizes both H- and K-Ras oncogenic signaling. FTI-277 TFA can inhibit hepatitis delta virus (HDV) infection.
    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-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
  • 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
Cat. No. Product Name / Synonyms Application Reactivity