Fatty Acid Synthase

Denifanstat (FASN-IN-2) is a Fatty Acid Synthase (FASN) inhibitor(IC50 of 0.052 μM and an EC50 of 0.072 μM),with potential antineoplastic activity.

TVB-3664 significantly decreases tubulin palmitoylation and mRNA expression. TVB-3664 is a reversible and highly bioavailable fatty acid synthase inhibitor (IC50: 18 nM and 12 nM for human and mouse cell palmitate synthesis, respectively).

VY-3-135 is a metastasis inhibitor and an acetyl-CoA synthetase 2 (ACSS2) modulator.

1. Pseudoprotodioscin has moderate cytotoxicity.

Orlistat (Tetrahydrolipstatin) is an Intestinal Lipase Inhibitor. The mechanism of action of orlistat is as a Lipase Inhibitor.

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.

Fas C-Terminal Tripeptide Acetate shows inhibitory activity of Fas/FAP-1 binding.

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 is an inhibitor of sterol regulatory element-binding proteins (SREBPs). It can also significantly up-regulate CYP3A4 expression and activity via the PXR-mediated pathway.

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.

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

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.

Trimetazidine dihydrochloride (Vastarel F) can improve myocardial glucose utilization by inhibiting fatty acid metabolism. Trimetazidine is the first cytoprotective anti-ischemic agent, also used as a vasodilator in ischemic heart disease or angina.

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.

FGH10019 is a novel inhibitor of sterol regulatory element-binding protein (SREBP) ( IC50 :1 μM).

Gallocatechin gallate has strong antioxidative, and anti-obesity activities, it inhibits 3T3-L1 differentiation and lipopolysaccharide induced inflammation through MAPK and NF-κB signaling; it also may have anti-diabetic effects by increasing sensitivity

FAS-IN-1 Tosylate is an effective fatty acid synthase inhibitor;Has an IC50 of 10 nM.

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.

UCM05 (G28UCM) is a potent inhibitor of fatty acid synthase (FASN) with efficacy against HER2+ breast cancer xenografts, including in 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].

L-Carnitine (L(-)-Carnitine) is an amino acid derivative. L-Carnitine facilitates long-chain fatty acid entry into mitochondria, delivering substrate for oxidation and subsequent energy production. Fatty acids are utilized as an energy substrate in all tissues except the brain.

Cerulenin is a natural inhibitor of fatty acid synthase (FAS). It is produced by the fungus Cephalosporium caeruleus.

BI99179 is a potent and selective type I fatty acid synthase (FAS) inhibitor with an IC50 of 79 nM and it exhibits significant exposure (both peripheral and central) upon oral administration in rats[1].

A-769662 is an effective, reversible AMPK activator(EC50=0.8 μM).

Isoscoparin is derived from Gentiana algida Pall with antioxidant and anti-adipogenic activities. Isoscoparin can be used in stuides about the prevention and treatment of obesity.

Pedunculoside is extracted from Ilex rotunda Thunb.

Beta-Hydroxyisovalerylshikonin is an inhibitor of protein-tyrosine kinases such as v-Src and EGFR, and has been shown to induce apoptosis in several human tumor cell lines. Beta-Hydroxyisovalerylshikonin significantly decreased viability of HCT116 cells (IC50 values = 30.9 μg/mL).

Albaspidin-AP, -PP, -PB inhibit Fatty acid synthase (FAS) with IC50 values ranging from 23.1+/-1.4 to 71.7+/-3.9 microM, they could be considered to be a promising class of FAS inhibitors, and FAS is emerging as a potential therapeutic target to treat can

Dihydrocurcumin is the main metabolite of curcumin, which can reduce fat accumulation and oxidative stress response. Dihydrocurcumin can regulate the mRNA and protein expression levels of SREBP-1C, PNPLA3 and PPARα, increase the protein expression levels of pAKT and PI3K, and reduce the intracellular NO and ROS contents through Nrf2 signaling pathway.

1. Desoxyrhaponticin (Deoxyrhaponticin) is an agent that is potentially effective in controlling postprandial hyperglycemia in diabetes, the in vivo antidiabetic action of this compound can be explained, in part at least, by inhibition of glucose transport in the small intestine and inhibition of glucose reabsorption in the kidney. 2. Desoxyrhaponticin and rhaponticin could be considered as promising fatty acid synthase(FAS) inhibitors, they could inhibit intracellular FAS activity and downregulate FAS expression in human breast cancer MCF-7 cells.

IPI-9119 is an orally active, selective and irreversible FASN inhibitor (IC50 = 0.3 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.

Ac-CoA Synthase Inhibitor1 (ACSS2 inhibitor) is the most potent and specific inhibitor of acetate-dependent acetyl-CoA synthetase 2 (ACSS2).

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

ACSS2-IN-2 (MTB-9655) is an inhibitor of acyl-CoA synthetase short-chain family member 2 (ACSS2). ACSS2-IN-2 can inhibit ACSS2 activity with an IC50 value of 3.8 nM. ACSS2-IN-2 can be used for the research of several diseases, such as viral infection, metabolic disorders, neuropsychiatric diseases, inflammatory/autoimmune conditions and cancer.

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.

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

Rimiducid is a lipid-permeable tacrolimus analogue, homodimerizing an analogue of human protein fkbp12 and binding to wild-type fkbp12 with 1000-fold lower affinity. Rimiducid is a dimerizer agent that acts by cross-linking the FKBP domains. It dimerizes the Caspase 9 suicide switch and rapidly induces apoptosis.

(-)-Hydroxycitric acid (HCA) can inhibit fat synthesis and reduces food intake, the primary mechanism of action of HCA appears to be related to its ability to act as a competitive inhibitor of the enzyme ATP-citrate lyase, which catalyzes the conversion of citrate and coenzyme A to oxaloacetate and acetyl coenzyme A (acetyl-CoA), primary building blocks of fatty acid and cholesterol synthesis.

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

Pyrazinamide (Pyrazinecarboxamide), an antimycobacterial, is utilized therapeutically as an antitubercular agent, which is a synthetic pyrazinoic acid amide derivative.

1β-Hydroxy-2-oxopomolic acid inhibits adipocyte differentiation through downregulation of various adipocytokines by blocking PPARγ and C/EBPα expression.

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).

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.