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-15879
    LB42708
    		Inhibitor ≥99.0%
    LB42708 is a potent, selective and orally active farnesyltransferase inhibitor. LB42708 inhibits farnesylation of H-Ras, N-Ras and K-Ras4B with IC50s of 0.8 nM, 1.2 nM and 2.0 nM, respectively.
    LB42708
  • HY-119257
    ABT-100
    		Inhibitor 98.18%
    ABT-100 is a potent, highly selective and orally active farnesyltransferase inhibitor. ABT-100 inhibits cell proliferation (IC50s of 2.2 nM, 3.8 nM, 5.9 nM, 6.9 nM, 9.2 nM, 70 nM and 818 nM for EJ-1, DLD-1, MDA-MB-231, HCT-116, MiaPaCa-2, PC-3, and DU-145 cells, respectively), increases apoptosis and decreases angiogenesis. ABT-100 possesses broad-spectrum antitumor activity.
    ABT-100
  • HY-123242A
    FTI-2153 TFA
    		Inhibitor 99.11%
    FTI-2153 TFA is a potent and highly selective inhibitor of farnesyltransferase (FTase), with an IC50 of 1.4 nM. FTI-2153 TFA is >3000-fold more potent at blocking H-Ras (IC50, 10 nM) than Rap1A processing. Anti-cancer activity.
    FTI-2153 TFA
  • HY-10502A
    Tipifarnib (S enantiomer)
    		99.52%
    Tipifarnib S enantiomer is the S-enantiomer of Tipifarnib. Tipifarnib is a potent and specific farnesyltransferase (FTase) inhibitor with IC50 of 0.6 nM. Tipifarnib S enantiomer is the less active isomer.
    Tipifarnib (S enantiomer)
  • HY-15873
    FTI 276
    		Inhibitor
    FTI-276 is a protein farnesyl transferase (PFT) inhibitor with IC50s of 0.9 and 0.5 nM for Plasmodium falciparum and human.
    FTI 276
  • HY-15872
    FTI-277
    		Inhibitor
    FTI-277 is an inhibitor of farnesyl transferase (FTase); a highly potent Ras CAAX peptidomimetic which antagonizes both H- and K-Ras oncogenic signaling. FTI-277 can inhibit hepatitis delta virus (HDV) infection.
    FTI-277
  • HY-118916A
    FTI-2148 diTFA
    		Inhibitor
    FTI-2148 diTFA 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 diTFA
  • HY-116254
    L-739750
    		Inhibitor
    L-739750 is a selective protein farnesyltransferase (PFTase) inhibitor (IC50: 0.4 nM). PFTase utilizes farnesyl diphosphate to farnesylate the cysteine residue of protein substrates having a C-terminal CAAX motif. L-739750 is a selective CAAX peptidomimetic.
    L-739750
  • HY-120763
    LB42908
    		Inhibitor
    LB42908 is a potent, selective and orally active farnesyltransferase inhibitor. LB42908 inhibits farnesylation of H-Ras, K-Ras with IC50 values of 0.9 nM, 2.4 nM for H-Ras, K-Ras, respectively. LB42908 shows antiproliferative activity. LB42908 shows antitumor activity.
    LB42908
  • 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-149015
    FTase-IN-1
    		Inhibitor
    FTase-IN-1 (compound 17a) is a potent and specific inhibitor of fanesyl transferase (FTase) with an IC50 of 0.35 μM. FTase-IN-1 displays cytotoxicity potential and antitumor activity.
    FTase-IN-1
  • HY-149016
    Tubulin polymerization-IN-25
    		Inhibitor
    Tubulin polymerization-IN-25 (compound 17f) is a dual inhibitor of tubulin polymerization and farnesyl transferase (FTase) with IC50s of 1.11 μM and 0.39 μM, respectively. Tubulin polymerization-IN-25 displays cytotoxicity and excellent antitumor activity .
    Tubulin polymerization-IN-25
  • 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 a selective squalene synthase inhibitor, which inhibits rat liver microsomal squalene synthase with an IC50 of 0.8 nM.
    RPR107393 free base
  • HY-16108A
    Squalene synthase-IN-3 tripotassium
    		Inhibitor
    Squalene synthase-IN-3 tripotassium (Compound 1) is a potent squalene synthase inhibitor.
    Squalene synthase-IN-3 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-N7634
    Tectol
    		Inhibitor 98.32%
    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
Cat. No. Product Name / Synonyms Application Reactivity