Farnesyl Transferase
Farnesyltransferase is one of the three enzymes in the prenyltransferase group. Farnesyltransferase's targets include members of the Ras superfamily of small GTP-binding proteins critical to cell cycle progression.
Farnesyltransferase inhibitors (FTIs) are small-molecule inhibitors that selectively inhibit farnesylation of a number of intracellular substrate proteins such as Ras. Farnesyl transferase inhibitors (FTIs) represent a new class of signaling inhibitors that is emerging in the clinical arena of hematologic malignancies and that may inhibit critical growth and survival signals. FTIs are a class of experimental cancer drugs that target protein farnesyltransferase with the downstream effect of preventing the proper functioning of the Ras (protein), which is commonly abnormally active in cancer.
Targets for Farnesyl Transferase
Products for Farnesyl Transferase
- Cat.No. Product Name Information
- GC60548 ABT-100 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.
- GC32865 BMS-214662 A potent FTase inhibitor
- GC62276 CP-609754 CP-609754 (LNK-754) is a potent and reversible farnesyltransferase inhibitor with potential anticancer activity.The IC50 for inhibiting farnesylation of recombinant human H-Ras is 0.57 ng/mL and recombinant K-Ras is 46 ng/mL.
- GC36038 FGTI-2734 FGTI-2734 is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC50s of 250 nM and 520 nM for FT and GGT-1, respectively. FGTI-2734 can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors.
- GC33367 FTI 276 FTI-276 is a protein farnesyl transferase (PFT) inhibitor with IC50s of 0.9 and 0.5 nM for Plasmodium falciparum and human.
- GC36085 FTI 276 TFA FTI-276 is a protein farnesyl transferase (PFT) inhibitor with IC50s of 0.9 nM and 0.5 nM for Plasmodium falciparum and human, respectively.
- GC16310 FTI 277 HCl FTI 277 HCl is an inhibitor of farnesyl transferase (FTase); a highly potent Ras CAAX peptidomimetic which antagonizes both H- and K-Ras oncogenic signaling.
- GC60861 FTI-2153 FTI-2153 is a potent and highly selective inhibitor of farnesyltransferase (FTase), with an IC50 of 1.4 nM. FTI-2153 is >3000-fold more potent at blocking H-Ras (IC50, 10 nM) than Rap1A processing. Anti-cancer activity.
- GC61775 FTI-2153 TFA 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.
- GC36086 FTI-277 FTI-277 is an inhibitor of farnesyl transferase (FTase); a highly potent Ras CAAX peptidomimetic which antagonizes both H- and K-Ras oncogenic signaling.
- GC32759 L-778123 hydrochloride (L-778,123 hydrochloride) L-778123 hydrochloride (L-778,123 hydrochloride) is an inhibitor of FPTase and GGPTase-I with IC50 of 2 nM and 98 nM in enzyme inhibition determination.
- GC38807 Lapaquistat acetate Lapaquistat acetate (TAK-475) is a squalene synthase inhibitor, blocking the conversion of farnesyl diphosphate (FPP) to squalene in the cholesterol biosynthesis pathway.
- GC31242 LNK754 LNK754 is the racemate of CP-609754.
- GC10330 Lonafarnib A farnesyltransferase inhibitor with antitumor activity
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GC10265
Manumycin A
farnesyltransferase inhibitor
- GC31276 Prenyl-IN-1 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.
- GC31556 RPR107393 free base RPR107393 free base is a selective squalene synthase inhibitor, which inhibits rat liver microsomal squalene synthase with an IC50 of 0.8 nM.
- GC61318 Tectol Tectol, isolated from Lippia sidoides, exhibits significant activity against human leukemia cell lines HL60 and CEM.
- GC15442 Tipifarnib (Zarnestra) A farnesyltransferase inhibitor with antitumor activity
- GC33007 Tipifarnib S enantiomer ((S)-(-)-R-115777) 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.
- GC31516 YM-53601 free base YM-53601 free base, a squalene synthase inhibitor, reduces plasma cholesterol and triglyceride levels in vivo.