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.

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.

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

FASN-IN-6 (compound 44), a potent fatty acid biosynthesis (FAB) inhibitor, serves as an antibacterial agent, exhibiting minimum inhibitory concentrations (MICs) of 1 μg mL for S. aureus ATCC 25923 and 4 μg mL for E. faecalis ATCC 29212 [1].

FASN-IN-4 tosylate is a potent fatty acid synthase (FASN) inhibitor with an IC50 of 10 nM and also exhibits inhibitory activity against SARS-CoV-2, with an EC50 of 18.6 nM [2].

FASN-IN-5 is a FASN inhibitor used in cancer and metabolic disease research.

FAS-IN-1 is a potent inhibitor of Fatty acid synthase (FAS) wtih IC50 of 10 nM.

Fasnall, a fatty acid synthase (FASN) inhibitor, exhibits an IC50 of 3.71 μM against the human recombinant enzyme. It halts tritiated acetate incorporation into lipids (IC50= 5.84 μM), boosts ceramide levels, and triggers lipid droplet formation in BT474 HER2+ breast cancer cells. Demonstrating antiproliferative effects on various breast cancer cell lines, including non-tumorigenic MCF-10A and tumorigenic MCF-7, MDA-MB-468, BT474, and SK-BR-3, its efficacy is directly linked to FASN expression in vitro. In murine models of HER2+ breast cancer, particularly the MMTV-Neu model, Fasnall significantly reduces tumor volume and extends survival. Furthermore, it enhances the efficacy of carboplatin in vivo, bolstering the objective response rate of stable disease from 25% with carboplatin alone to 88% when paired with Fasnall.

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

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.

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.

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.

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.

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

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.

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

Fatostatin is a specific inhibitor of SREBP activation, it impairs the activation of SREBP-1 and SREBP-2. Fatostatin binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs.

Fatostatin hydrobromide (Fatostatin A HBr) ia an inhibitor of sterol regulatory element binding protein (SREBP). It impairs the activation of SREBP-1 and SREBP-2.

Morin (Calico Yellow) was found to be a weak inhibitor of fatty acid synthase (IC50: 2.33 μM). Morin is a yellow color substance that can be isolated from Maclura pomifera (Osage orange), Maclura tinctoria (old fustic) and from leaves of Psidium guajava (common guava).

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.

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

Icariside E4 is a natural compound derived from Ulmus minor that acts via AMPK phosphorylation and inhibition of MID1IP2 hypolipidation in HepG1 cells.Icariside E4 has anti-injurious, antioxidant, anti-Alzheimer's and anti-inflammatory effects and inhibits SREBP-1c, liver X receptor-α (LXR) and FASN in Icariside E4 is an effective candidate for the treatment of fatty liver disease and has hypolipidemic potential in HepG1 cells.

CTL-12, a fatty acid synthase (FASN) inhibitor (IC50: 2.5 μM), induces apoptosis and disrupts the cell cycle at the Sub-G1 S phase. It upregulates caspase-9 and the apoptosis marker Bax, while downregulating the anti-apoptotic marker Bcl-xL. By inhibiting de novo lipogenesis, CTL-12 thwarts tumor cells' metabolic requirements and is frequently employed in breast and colorectal cancer studies [1].

PFM046 is an antagonist of the liver X receptor (LXR), effectively inhibiting the activation of LXRα and LXRβ, with IC50 values of 2.04 μM and 1.58 μM respectively. It reduces the expression of SCD1 and FASN while increasing ABCA1 expression, and demonstrates antitumor activity in mouse models.