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Fatty acid synthase (FASN) inhibitors block the enzyme that assembles palmitate from acetyl and malonyl units. FASN is a large homodimeric protein that carries all catalytic steps of fatty acid synthesis on one polypeptide chain. Many tumor cells express high FASN levels and rely on de novo lipogenesis, so the enzyme is studied in cancer metabolism. C75, a synthetic α-methylene-γ-butyrolactone, was described in 2000 as a FASN inhibitor tested in xenografts. Orlistat, known as a pancreatic lipase inhibitor, was shown in 2004 to inhibit the thioesterase domain of FASN. Denifanstat, TVB-3166 and TVB-3664 are later reversible FASN inhibitors from a related chemical series. The list also includes natural products reported to inhibit FASN, such as dihydrocurcumin and praeruptorin B.
Synonyms: Tetrahydrolipstatin
Orlistat is a general lipase inhibitor with IC50 of 122 ng/ml for PL from human duodenal juice. Orlistat is also an inhibitor of fatty acid synthase (FASN), is used orally for long-term research of obesity. Anti-atherosclerotic effect.
Synonyms: C75
C 75 is an inhibitor of fatty acid synthase (FAS) reducing food intake and body weight in mice.
Synonyms: FASN-IN-2; TVB-2640
Denifanstat (TVB-2640) is a Fatty Acid Synthase (FASN) inhibitor extracted from patent WO2012122391A1, compound 152, has an IC50 of 0.052 μM and an EC50 of 0.072 μM.
C75 is a novel, potent synthetic inhibitor of fatty acid synthase (FAS), which is used as a tool for studying fatty acid synthesis in metabolic disorders and cancer.
Synonyms: Praeruptorin D
Praeruptorin B is an inhibitor of fatty acid synthase (FASN), which plays a critical role in lipid metabolism. This compound demonstrates significant anti-lipogenic activity, making it a valuable tool for studying metabolic disorders and cancer biology. It can be utilized in research applications focused on the regulation of lipid synthesis and its associated pathways.
Dihydrocurcumin, a key metabolite of curcumin, acts as a fatty acid synthase (FASN) inhibitor. It is known to decrease lipid accumulation and oxidative stress by modulating the expression of key regulatory proteins such as SREBP-1C, PNPLA3, and PPARα. Additionally, Dihydrocurcumin enhances the protein levels of pAKT and PI3K while diminishing cellular nitric oxide (NO) and reactive oxygen species (ROS) through involvement in Nrf2 signaling pathways. This compound is valuable for investigating lipid metabolism and oxidative stress in various biological contexts.
Synonyms: TVB3166.
TVB-3166 is an orally-available, reversible, potent, and selective FASN inhibitor, inducing apoptosis, inhibiting anchorage-independent cell growth under lipid-rich conditions, and inhibiting in-vivo xenograft tumor growth.
Synonyms: TVB3664.
TVB-3664 is an orally available, reversible, potent, selective and highly bioavailable fatty acid synthase (FASN) inhibitor, with IC50 values of 18 nM and 12 nM for human and mouse cell palmitate synthesis, respectively. TVB-3664 significantly reduces tubulin palmitoylation and mRNA expression.
FT113 is a potent and orally active fatty acid synthase (FASN) inhibitor, with an IC50 of 213 nM for full-length recombinant human FASN enzyme.
FASN-IN-1 is a fatty acid synthase (FASN) inhibitor extracted from patent WO2015134790A1, compound 56.
HS-79 is an enantiomer of Fasnall, which is a selective fatty acid synthase (FASN) inhibitor. HS-79 is able to inhibit the incorporation of tritiated acetate into lipids with an IC50 of 1.57 μM.
Desoxyrhaponticin is a stilbene glycoside from the Tibetan nutritional food Rheum tanguticum Maxim. Desoxyrhaponticin is a Fatty acid synthase (FAS) inhibitor, and has apoptotic effect on human cancer cells.
HS-80 is an enantiomer of Fasnall, which is a selective fatty acid synthase (FASN) inhibitor. HS-80 is able to inhibit the incorporation of tritiated acetate into lipids with an IC50 of 7.13 μM.
GSK2194069 is a potent and specific inhibitor of the β-ketoacyl reductase (KR) activity of hFAS with an IC50 of 7.7 ± 4.1 nM in an assay detecting released CoA.
Lycorine is a natural alkaloid extracted from the Amaryllidaceae plant. Lycorine is a potent and orally active SCAP inhibitor with a Kd value 15.24 nM.
Fasnall is a selective inhibitor of fatty acid synthase (FASN), exhibiting an IC50 of 3.71 μM. This compound effectively induces apoptosis in HER2+ breast cancer cell lines, demonstrating significant anti-tumor activity. Fasnall serves as a valuable tool in cancer research, particularly in exploring metabolic pathways and therapeutic strategies for targeting FASN in oncology.
Fasnall benzenesulfonate is a selective inhibitor of fatty acid synthase (FASN), exhibiting an IC50 value of 3.7 μM. This compound effectively reduces cell proliferation and induces apoptosis in breast cancer cells, demonstrating its potential as an antitumor agent. Additionally, Fasnall benzenesulfonate has shown significant antitumor efficacy in in vivo models, supporting its application in cancer research and therapeutic development.
Synonyms: G28UCM
UCM05 is a potent inhibitor of fatty acid synthase (FASN) and Filamentous temperature-sensitive protein Z (FtsZ). This compound demonstrates significant anti-cancer activity against HER2+ breast cancer xenografts and retains efficacy in drug-resistant cell lines. Additionally, UCM05 exhibits inhibitory effects on the growth of the Gram-positive bacterium Bacillus subtilis, with a minimum inhibitory concentration (MIC) of 100 μM, while showing no activity against the Gram-negative bacterium Escherichia coli. This dual-targeting capability makes UCM05 useful in cancer research and microbiology studies.
FASN-IN-4 tosylate is a highly effective inhibitor of fatty acid synthase (FASN), exhibiting an IC50 value of 10 nM. In addition to its role as a FASN inhibitor, this compound has demonstrated antiviral activity against SARS-CoV-2, with an EC50 of 18.6 nM. FASN-IN-4 tosylate is relevant for research applications aimed at exploring metabolic pathways and developing antiviral strategies.
FASN-IN-7 is a potent inhibitor of human Fatty Acid Synthase (FASN), with IC50 values of 28 nM for full-length FASN and 54 nM for the FASN KR domain. This compound effectively inhibits the proliferation of various cancer cell types and alters lipid metabolism by increasing malonyl-CoA levels while reducing palmitate levels in tumor tissues. FASN-IN-7 serves as a valuable tool for researching metabolic pathways in cancer biology and the potential therapeutic modulation of FASN activity.
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IPI-9119 is a selective and irreversible inhibitor of Fatty Acid Synthase (FASN), exhibiting an IC50 of 0.3 nM in in vitro assays. This compound demonstrates significant anti-tumor activity in castration-resistant prostate cancer (CRPC) xenograft models, highlighting its potential for therapeutic applications in the treatment of advanced prostate cancer. Researchers may utilize IPI-9119 to investigate the role of FASN inhibition in cancer metabolism and therapeutic resistance.
FASN-IN-5 is a selective inhibitor of fatty acid synthase (FASN), primarily targeting lipid metabolism pathways. It demonstrates significant biological activity in modulating TH17- and CSF1-mediated disease mechanisms, including various cancers, immunological disorders, and obesity. This compound serves as a valuable tool for researchers investigating FASN-related pathways in disease progression and therapeutic interventions.
GSK837149A is a selective inhibitor of human Fatty Acid Synthase (FASN), specifically targeting the KR domain. It exhibits reversible inhibition with a high affinity for type I FASN (Ki = 30 nM), functioning as a competitive inhibitor of NADPH and a non-competitive inhibitor of acetoacetyl-CoA. GSK837149A is applicable in research exploring obesity and breast cancer, providing valuable insights into metabolic regulation and tumorigenesis.
FASN-IN-3 is a potent inhibitor of fatty acid synthase (FASN), a critical enzyme in lipid biosynthesis. This compound is particularly useful for investigating the role of FASN in metabolic disorders and cancer, where altered fatty acid metabolism is a key feature. Research applications include studies on cellular proliferation and survival in FASN-dependent cancer cell lines, as well as assays evaluating the impact of lipid synthesis inhibition on cellular signaling pathways.
(−)-C75 is a synthetic inhibitor of fatty acid synthase (FASN) that effectively inhibits the growth of prostate cancer cells, such as PC3, with an IC50 of 35 µM. Additionally, (−)-C75 acts as a potent activator of carnitine palmitoyltransferase 1A (CPT1A). This compound is valuable for research applications focused on cancer metabolism and therapeutic strategies targeting lipid biosynthesis.
