fatty acid synthase (fasn)

Denifanstat (FASN-IN-2) is a fatty acid synthase (FASN) inhibitor (IC50=0.052 μM, EC50=0.072 μM) with selective and oral activity. Denifanstat has been used in studies of steatohepatitis.

TVB-3664 is an orally active, selective, reversible, and highly bioavailable fatty acid synthase inhibitor (FASN) with an IC50 for palmitate synthesis of 18 nM in human and 12 nM in mouse.Significantly inhibits microtubule protein palmitoylation and mRNA expression.

FASN-in-1 is an effective, specific inhibitor of fatty acid synthase (FASN), a compound specifically designed to target and inhibit the activity of the enzyme involved in fatty acid synthesis, potentially disrupting fatty acid production and affecting various cellular processes.

Praeruptorin B (Praeruptorin D), a compound found in the roots of Peuced, is an inhibitor of sterol regulatory element-binding proteins (SREBPs) that attenuates the metastatic ability of human renal cancer cells by targeting CTSC and CTSV expression, and can be used in the study of osteoporosis.

Orlistat (Tetrahydrolipstatin) is a lipase inhibitor and a fatty acid synthase (FASN) inhibitor. Orlistat has been shown to promote weight loss.

Betulin (betulinol) (lup-20(29)-ene-3β, 28-diol) is an abundant, naturally occurring triterpene. It is commonly isolated from the bark of birch trees where it forms up to 30% of the dry weight of the extractive and is found in birch sap as well.

trans-Chalcone (Chalkone) is an aromatic ketone that forms the central core for a variety of important biological compounds, which are known collectively as chalcones.

Lycorine (Narcissine) inhibits protein synthesis and may inhibit ascorbic acid biosynthesis, although studies on the latter are controversial and inconclusive.

Eicosapentaenoic Acid is an ω-3 fatty acid and an inhibitor of fatty acid synthase (FASN). Eicosapentaenoic Acid promotes DNA demethylation in the reexpression of the tumor suppressor gene CCAAT/ enhancer-binding protein δ (C/EBPδ). Eicosapentaenoic Acid activates the RAS/ERK/C/EBPβ pathway in U937 leukemia cells through demethylation of the CpG island of H-RAS intron 1. Eicosapentaenoic Acid promotes the relaxation of vascular smooth muscle cells and vasodilation.

FASN-IN-3 is an inhibitor of fatty acid synthase (FASN).

FT113 is a novel potent inhibitor of fatty acid synthase (fasn, IC50 : 213 nM),and exhibits anti-cancer activity

trans-C75 ((±)-C75) is an enantiomer of C75, which is an inhibitor of fatty-acid synthase (FASN).

C75 is an inhibitor synthetic fatty-acid synthase (FASN) and inhibits prostate cancer cells PC3 (IC50: 35 μM).C75 increases CPT1 activity and reduces DIO.

HS-79, an enantiomer of Fasnall, is a selective fatty acid synthase (FASN) inhibitor that inhibits the incorporation of tritiated acetate into lipids (IC50: 1.57 μM).

HS-80, an enantiomer of Fasnall, is a selective fatty acid synthase (FASN) inhibitor that inhibits the incorporation of tritiated acetate into lipids (IC50: 7.13 μM).

PF429242 dihydrochloride is a reversible and competitive inhibitor of S1P, with an IC50 of 175 nM.

GSK2194069 is an active β-keto reductase (KR)-specific inhibitor of fatty acid synthase (FASN) with an IC50 of 7.7 nM in an assay for the detection of released CoA.GSK2194069 inhibits the proliferation of FAS in cancer cells through the action of acetoacetyl-coenzyme A and NADPH.

TVB-3166 induces apoptosis and inhibits in-vivo xenograft tumor growth. TVB-3166 is a reversible and selective fatty acid synthase inhibitor (IC50s: 42 nM and 81 nM for biochemical FASN and cellular palmitate synthesis, respectively).

Octyl Orlistat, a potential fatty acid synthase (FASN) inhibitor, has demonstrated significant effectiveness in reducing tumor cell proliferation. By targeting FASN and inducing apoptosis, Orlistat is under investigation as an anti-tumor compound. Compared to Cerulenin and C75, Orlistat shows greater inhibitory potency in cell culture and cell lines. In LN229 cells, treatment with 200 µM Orlistat for 48 hours resulted in a 63.9 ± 8.7% reduction in cell growth, while in LT68 cells, the reduction was 76.3 ± 23.7%. Organotypic slice cultures treated with Orlistat exhibited decreased proliferation after Ki67 staining and an increase in caspase-3 cleavage.

Decyl-Plastoquinone exhibits inhibitory activity against the thioesterase domain of fatty acid synthase (FASN), demonstrating anticancer potential.

QNX-10 is a fatty acid synthase (FASN) inhibitor with anticancer properties (IC50 = 0.7 μM). It exhibits potent FASN inhibition and cytotoxicity against colorectal and breast cancer cells. By upregulating the pro-apoptotic protein Bax and downregulating the anti-apoptotic protein Bcl-xL, QNX-10 induces apoptosis and causes cell cycle arrest at the S phase. This compound is utilized for investigating anticancer therapies targeting the FASN enzyme.

FASN/SCD-IN-1 is a Silybin derivative and an orally active inhibitor of fatty acid synthase (FASN) and stearoyl-CoA desaturase (SCD). In vitro, FASN/SCD-IN-1 demonstrates the ability to inhibit lipid deposition, reduce the transcription levels of FASN and SCD, and exhibits antioxidant, anti-inflammatory, and antifibrotic activities. It shows significant hepatoprotective effects in rat models of acute liver injury and improves pathological features such as steatosis, inflammation, and fibrosis in a mouse model of myeloproliferative-associated steatohepatitis (MASH). FASN/SCD-IN-1 can be used for MASH research.

UCM05 (G28UCM) is a potent inhibitor of fatty acid synthase (FASN) with efficacy against HER2+ breast cancer xenografts, including cell lines resistant to anti-HER2 drugs [1]. Additionally, it functions as an inhibitor of the Filamentous temperature-sensitive protein Z (FtsZ), selectively inhibiting the growth of the Gram-positive bacterium B. subtilis with minimum inhibitory concentration (MIC) values of 100 μM, while showing no activity against the Gram-negative bacterium E. coli [2].

Fasnall is a selective FASN inhibitor that acts through its co-factor binding sites. Fasnall shows potent anti-tumor activity in the MMTV-Neu model of HER2(+) breast cancer, particularly when combined with carboplatin.