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.
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Farnesyl Transferase Related Products (97)
Related Products (97)
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Antibodies (1)
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FGTI-2734 mesylate
0 ImagesFGTI-2734 mesylate is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT) inhibitor with IC50s of 250 nM and 520 nM for FT and GGT, respectively. FGTI-2734 mesylate can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors.
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Psammaplin A
0 ImagesCat. No.: HY-N2150CAS No.: 110659-91-1Psammaplin A is a marine metabolite. Psammaplin A is a selective HDAC1 (IC50: 45 nM), DNA methyltransferases (IC50: 18.6 nM) and aminopeptidase N (APN) (IC50: 18 μM) inhibitor. Psammaplin A also inhibits DNA topoisomerase and farnesyl protein transferase. Psammaplin A is a PPARγ activator and induces apoptosis. Psammaplin A has antitumor and anti-inflammatory activities. Psammaplin A has antibacterial activity against Gram-positive bacteria and inhibits DNA synthesis and DNA gyrase activity. Psammaplin A inhibits angiogenesis.
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FTI 276 TFA
0 ImagesFTI 276 TFA is a farnesyltransferase (FTase) inhibitor with an IC50 of 0.5 nM, and it exhibits selectivity for FTase over geranylgeranyltransferase I (GGTase I). FTI 276 TFA blocks the farnesylation of H-Ras and K-Ras4B, causes inactive Ras-Raf complexes to accumulate in the cytoplasm, and inhibits constitutive MAPK activation. FTI 276 TFA reduces the number, incidence and volume of tumors, and restricts the growth of tumors expressing activated K-ras. FTI 276 TFA can be used in research related to pulmonary adenoma.
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ABT-100
0 ImagesCat. No.: HY-119257CAS No.: 450839-40-4ABT-100, a chemical probe, 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.
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Darlifarnib
0 ImagesCat. No.: HY-172423CAS No.: 3065226-39-0Synonyms: KO-2806Darlifarnib (KO-2806) is an orally active farnesyl transferase inhibitor. Darlifarnib inhibits the mTORC1 signaling pathway, thereby enhancing the anti-angiogenic properties of tyrosine kinase inhibitors. When used in combination with anti-VEGFR tyrosine kinase inhibitors, Darlifarnib promotes renal cell carcinoma tumor regression and inhibits tumor neovascularization. Darlifarnib sensitizes renal cell carcinoma tumors that progress after anti-VEGFR TKI treatment.
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BMS-214662 hydrochloride
0 ImagesBMS-214662 hydrochloride is an inhibitor of farnesyltransferase (Farnesyl Transferase). BMS-214662 hydrochloride can effectively block the localization and function of Ras proteins on the cell membrane by inhibiting the prenylation modification of Ras proteins, thereby exerting anti-tumor activity. The IC50 value of BMS-214662 hydrochloride for H-Ras is 1.3 nM, and for K-Ras it is 8.4 nM. BMS-214662 hydrochloride can be used in the research of tumor diseases related to Ras.
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FTI 276
0 ImagesCat. No.: HY-15873CAS No.: 170006-72-1FTI-276 is a protein farnesyl transferase (PFT) inhibitor with IC50s of 0.9 and 0.5 nM for Plasmodium falciparum and human.
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Tectol
0 ImagesTectol, 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.
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Olpadronic acid
0 ImagesCat. No.: HY-106431CAS No.: 63132-39-8Synonyms: Olpadronate; OLPOlpadronic acid (Olpadronate) is an orally active amino-bisphosphonate and inhibits bone resorption. Olpadronic acid prevents bone destruction and tumor growth in the skeletal prostate cancer mouse model. Olpadronic acid can be used for research of osteoporosis, malignancies and rheumatoid arthritis.
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Tipifarnib (S enantiomer)
0 ImagesSynonyms: IND-58359 S enantiomer; (S)-(-)-R-115777Tipifarnib 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.
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FTI-277
0 ImagesCat. No.: HY-15872CAS No.: 170006-73-2FTI-277 is a farnesyltransferase (FTase) inhibitor. FTI-277 inhibits Ras farnesylation, blocks the phosphorylation of downstream ERK1/2 and mTOR, and reduces membrane-bound active N-ras protein. FTI-277 activates caspase 3, upregulates Bim expression, induces cell apoptosis, suppresses regulatory T cell expansion, enhances macrophage phagocytosis, and improves bacterial clearance. FTI-277 activates the PI3K/Akt signaling pathway, inhibits osteoblast differentiation, and reduces the proliferation ability of neuroblastoma cells. FTI-277 can be used in research related to head and neck squamous cell carcinoma, neuroblastoma, sepsis, and vascular calcification.
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(S)-(-)-Perillyl alcohol (Standard)
0 ImagesCat. No.: HY-116514RCAS No.: 18457-55-1(S)-(-)-Perillyl alcohol (Standard) is the analytical standard of (S)-(-)-Perillyl alcohol (HY-116514). This product is intended for research and analytical applications. (S)-(-)-Perillyl alcohol, a monoterpene, is an orally active farnesyl transferase and geranylgeranyl transferase inhibitor. (S)-(-)-Perillyl alcohol up-regulates the mannose-6-phosphate receptor, facilitating TGF-β1 activation and cytostasis,. (S)-(-)-Perillyl alcohol induces apoptosis in cancer cells, modulates cyclin D1 and AP-1 activity. (S)-(-)-Perillyl alcohol exhibits antitumor activity against sarcoma tumors in mice. (S)-(-)-Perillyl alcohol can be used for the research of squamous cell carcinoma of the esophagus and sarcoma 180.
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FTI-2148 diTFA
0 ImagesCat. No.: HY-118916ACAS No.: 817586-01-9FTI-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.
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L-739750
0 ImagesCat. No.: HY-116254CAS No.: 160141-08-2L-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.
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LB42908
0 ImagesCat. No.: HY-120763CAS No.: 226927-89-5
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A-228839
0 ImagesCat. No.: HY-16013CAS No.: 216234-25-2A-228839 is a potent farnesyltransferase inhibitor. A-228839 inhibits lymphocyte activation and cytokine production.
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FTase-IN-1
0 ImagesCat. No.: HY-149015CAS No.: 2490538-41-3FTase-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.
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Tubulin polymerization-IN-25
0 ImagesCat. No.: HY-149016CAS No.: 2490538-46-8Tubulin 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 .
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Squalene synthase-IN-2
0 ImagesCat. No.: HY-163452Squalene 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.
