Farnesyl Transferase Inhibitor

FTI-2628 is an antimalarial agent and a farnesyl transferase inhibitor, with an IC₅₀ of 41.7 nM against TbPET. FTI-2628 attenuates glucose-stimulated insulin secretion. FTI-2628 exhibits antimalarial activity against Trypanosoma brucei.

L-778123 dihydrochloride is a dual FPTase and GGPTase-I inhibitor, with IC₅₀s of 2 nM and 98 nM, respectively.

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.

E5700 is an orally active squalene synthase inhibitor, antimalarial agent and antifungal agent with an IC₅₀ of 0.49 nM (without PPi) against squalene synthase from T. cruzi epimastigotes. E5700 shows antiparasitic activities against Trypanosoma cruzi. E5700 inhibits the growth and alters the lipid prolife and the ultrastructure of a multiple agent-resistant C. tropicalis strain. E5700 is a potent and selective inhibitor of the growth of Leishmania amazonensis.

Andrastin D is a protein farnesyltransferase inhibitor. Andrastin D has a common androstane skeleton.

Gerfelin inhibits geranylgeranyl diphosphate synthase (GGPP synthase) activity with an IC₅₀ of 3.5 μg/mL.

FTI-277 TFA is a farnesyltransferase (FTase) inhibitor. FTI-277 TFA inhibits Ras farnesylation, blocks the phosphorylation of downstream ERK1/2 and mTOR, and reduces membrane-bound active N-ras protein. FTI-277 TFA activates caspase 3, upregulates Bim expression, induces cell apoptosis, suppresses regulatory T cell expansion, enhances macrophage phagocytosis, and improves bacterial clearance. FTI-277 TFA activates the PI3K/Akt signaling pathway, inhibits osteoblast differentiation, and reduces the proliferation ability of neuroblastoma cells. FTI-277 TFA can be used in research related to head and neck squamous cell carcinoma, neuroblastoma, sepsis, and vascular calcification.

BMS-186511 is a farnesyltransferase (FT) inhibitor and shows anticancer activity.

Kurasoin B is a protein farnesyltransferase inhibitor (IC₅₀: 58.7 μM). Kurasoin B can be produced by Paecilomyces sp. FO-3684.

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.

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).

Aminobutane bisphosphonate is a Trypanosoma cruzi farnesyl pyrophosphate synthase (FPPS) inhibitor with an IC₅₀ of 30.77 μM against Trypanosoma cruzi. Aminobutane bisphosphonate inhibits proliferation of intracellular amastigote Trypanosoma cruzi and lacks activity against non-infective epimastigote forms. Aminobutane bisphosphonate reduces osteoclastic bone resorption, osteoid surface extent, and osteoclast number per mm of bone surface. Aminobutane bisphosphonate can be used for the research of american trypanosomiasis (chagas' disease) and immobilization-related bone loss.

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.

(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.