Farnesyl Transferase Inhibitor

BMS-187745 tripotassium (Compound 1) is a potent squalene synthase 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.

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.

BMS-214662 mesylate is a potent and selective farnesyl transferase inhibitor with an IC₅₀ of 1.35 nM. BMS-214662 mesylate exhibits potent antitumor activity and can be utilized in cancer research.

A-176120 is a selective inhibitor of farnesyl transferase (IC₅₀=1.2 nM) based on a farnesyl pyrophosphate (FPP) analog, with superior selectivity against GGTaseI (IC₅₀=423 nM), GGTaseII (IC₅₀=3000 nM), and SSase (IC₅₀>10 μM). A-176120 inhibits ras processing in H-ras transformed NIH3T3 cells and HCT116 K-ras mutant cells (ED₅₀=1.6 and 0.5 μM, respectively). A-176120 has antiangiogenic and antitumor activities in vivo and reduces capillary structure formation and VEGF secretion.

L-744832 is a farnesyl transferase inhibitor. L-744832 effectively inhibits the farnesylation of H-Ras and N-Ras, but has little effect on K-Ras treatment. L-744832 not only directly targets the oncogenic pathway by inhibiting Ras farnesylation, but also enhances radiosensitivity by restoring TGF-β signaling through epigenetic reprogramming. L-744832 can induce cell cycle arrest and apoptosis. L-744832 can be used in combination therapy studies for Ras-driven tumors such as pancreatic cancer.

Pepticinnamin E is a Farnesyltransferase (FTase) inhibitor (IC₅₀=42 µM). Pepticinnamin E can be used in cancer and malaria research.

L-731735 is a selective FPTase inhibitor that can inhibit ras-dependent cell transformation. L-731735 can be used in cancer research.

SQS-IN-1 is a squalene synthase (SQS) inhibitor. SQS-IN-1 exhibits potent and broad-spectrum anti-proliferative effects on both mouse and human lung cancer cell lines. SQS-IN-1 inhibits DNA replication and the cell cycle, causing mitochondrial hyperpolarization and inducing cell apoptosis. SQS-IN-1 inhibits cell migration and invasion. SQS-IN-1 can be used to the study of lung cancer.

Antifungal agent 46 (compound 2f) is a potent antifungal agent. Antifungal agent 46 prevents Ras signaling by inhibiting protein farnesyltransferase.

Ftase inhibitor III is an anion-dependent Farnesyltransferase inhibitor from a phenotypic screen.

YM-53601 free base, a squalene synthase inhibitor, reduces plasma cholesterol and triglyceride levels in vivo. YM-53601 free base inhibits squalene synthase derived from human hepatoma cells with an IC₅₀ of 79 nM. Lipid-lowering agent. YM-53601 free base is also an inhibitor of farnesyl-diphosphate farnesyltransferase 1 (FDFT1) enzyme activity and abrogates HCV propagation.

AZD3409 is a prenyl inhibitor that exhibits inhibitory activity against both farnesyl transferase and geranylgeranyl transferase I. AZD3409 inhibits the growth of breast cancer cells, with IC₅₀s of 220 nM (MDA-MB-468), 180 nM (MDA-MB-361), and 290 nM (SK-Br-3). AZD3409 significantly reduces the activation level of AKT in breast cancer cell lines. AZD3409 induces G0/G1 phase arrest in MDA-MB-468 cells, causes G2/M phase arrest in MDA-MB-361 cells. AZD3409 can be used for the study of breast cancer.

BPH252 (Compound 4) is a geranylgeranyl diphosphate synthase inhibitor. BPH252 can be used in research on bisphosphonate-based anticancer inhibitors.

BIM-46068 is a potent, selectively human brain Farnesyltransferase (FTase) inhibitor (IC₅₀ = 91.4 nM). BIM-46068 can specifically inhibit Ras processing in MiaPaCa-2 cancer cells. BIM-46068 can be used for the study of pancreatic cancer.

RPR107393 is an orally active potent selective squalene synthase (SQS) inhibitor. RPR107393 inhibits rat liver microsomal squalene synthase with an IC₅₀ value of 0.8 nM. RPR107393 reduces triglyceride biosynthesis by suppressing fatty acid biosynthesis via an increase in intracellular farnesol and its derivatives. RPR107393 reduces plasma cholesterol in rats and marmosets. RPR107393 can be used for metabolic disease research, such as hypercholesterolemia, hypertriglyceridemia and atherosclerosis.

(Rac)-Tipifarnib ((Rac)-IND 58359; (Rac)-R115777) is a potent farnesyl protein transferase inhibitor that specifically targets the pro-tailation process of Ras proteins. (Rac)-Tipifarnib showed significant in vivo antitumor effects after oral administration to mice.

Ftase inhibitor I (B581) is a potent, selective and peptidomimetic farnesyl transferase (FTase) inhibitor. Ftase inhibitor I shows selectivity for FTase over geranylgeranyl isoprenoid (Ras-GG) or the fatty acid myristate (Myr-Ras).

FPPS-IN-2 (compound 4a) is a potent and orally active HFPPS inhibitor with an IC₅₀ value of 1.108 µM. FPPS-IN-2 has the potential for the research of osteoporosis.

J-104118 is a potent and orally active squalene synthase (SQS) inhibitor with an IC₅₀ of 0.52 nM. J-104118 inhibits cholesterol synthesis in mice. J-104118 can be used for cholesterol-lowering research.