fasn

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-4 tosylate is a potent fatty acid synthase (FASN) inhibitor, exhibiting an IC50 value of 10 nM. Additionally, it demonstrates inhibitory activity against SARS-CoV-2, with an EC50 of 18.6 nM [2].

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].

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

FASN-IN-5 (example 11) is a FASN inhibitor that can be used in studies of TH17 or CSF1-mediated diseases or disorders (e.g. cancer, immune disorders, obesity).

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.

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.

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).

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

1. Pseudoprotodioscin has moderate cytotoxicity.

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.

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 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.

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).

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

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.

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

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).

Trans-Petroselinic acid, the trans isomer of petroselinic acid and an isomer of oleic acid, is detected in the milk fat of cows, goats, and ewes, as well as human breast milk. In HepG2 cells, when treated with trans-petroselinic acid (100 μM), there is an increase in the cellular content of triacylglycerols and cholesterol esters. Additionally, it upregulates the transcription of genes associated with fatty acid synthesis (SREBP-1c, ACACA, FASN, SCD1) and cholesterol synthesis (HMGCR, HMGCS1, FDFT1, SREBP-2).

CTL-06, a Fatty Acid Synthase (FASN) inhibitor with an IC50 of 3 μM, induces apoptosis, while CTL-12 impedes cell cycle progression in the Sub-G1/S phase and modulates apoptotic and anti-apoptotic markers by upregulating caspase-9 and Bax and downregulating Bcl-xL. Additionally, CTL-12 suppresses de novo lipogenesis, curtailing the metabolic needs of tumor cells, with utilization in breast and colorectal cancer studies [1].

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].

1. Agrimol B is a main active ingredient isolated from Agrimonia pilosa Ledeb.

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].

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

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 (IC50: 1.57 μM).

Pedunculoside is extracted from Ilex rotunda Thunb.

Orlistat-d3 is intended for use as an internal standard for the quantification of orlistat by GC- or LC-MS. Orlistat is a digestive lipase inhibitor. It inhibits diacylglycerol lipase α (DAGLα), DAGLβ, α/β-hydrolase domain-containing protein 12 (ABHD12), ABHD16A, and platelet-activating factor acetylhydrolase (PAF-AH; IC50s = 0.06, 0.1, 0.08, 0.03, and 0.05 µM, respectively), as well as pancreatic lipase and hormone-sensitive lipase (IC50s = 0.65 and 2.1 µg/ml, respectively) but does not inhibit fatty acid amide hydrolase (FAAH) or KIAA1363 (IC50s = >100 µM for both). Orlistat decreases ionomycin-induced production of the endocannabinoid 2-arachidonoyl glycerol (2-AG) in N18TG2 murine neuroblastoma cells when used at a concentration of 1 µM. It also inhibits fatty acid synthase (FASN; Kiapp = ~0.1 µM for the human enzyme) and the proliferation of PC3 prostate cancer cells in a concentration-dependent manner. Orlistat (10 mg/kg) decreases serum cholesterol levels and total bod......

PF429242 dihydrochloride is a reversible and competitive inhibitor of S1P (IC50 of 175 nM).

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

SR-1903 is a modulator of retinoic acid receptor-related orphan receptor γ (RORγ) and liver X receptor (LXR). It is an inverse agonist of RORγ and an agonist of LXR. It also binds to peroxisome proliferator-activated receptor γ (PPAR) but does not activate it. SR-1903 inhibits LPS-induced expression of triggering receptor expressed on myeloid cells 1 (TREM-1). It also inhibits LPS-induced expression of the LXR target genes IL-6 and IL-33 and increases expression of ABCG1, FASN, and SCD-1. SR-1903 reduces the severity of collagen-induced arthritis. It reduces blood glucose levels in a glucose tolerance test, serum levels of total cholesterol and LDL, body weight, and fat mass in a mouse model of high-fat diet-induced obesity.

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

SR 1903 is a modulator of retinoic acid receptor-related orphan receptor γ (RORγ) and liver X receptor (LXR).1 It is an inverse agonist of RORγ (IC50 = ~100 nM in a cell-based reporter assay) and an agonist of LXR. It also binds to peroxisome proliferator-activated receptor γ (PPARγ; IC50 = 209 nM) but does not activate it. SR 1903 (10 μM) inhibits LPS-induced expression of triggering receptor expressed on myeloid cells 1 (TREM-1) in RAW 264.7 cells. It also inhibits LPS-induced expression of the LXR target genes IL-6 and IL-33 and increases expression of ABCG1, FASN, and SCD-1 in RAW 264.7 cells. SR 1903 (20 mg/kg twice per day) reduces severity score in a mouse model of collagen-induced arthritis. It reduces blood glucose levels in a glucose tolerance test, serum levels of total cholesterol and LDL, body weight, and fat mass in a mouse model of high-fat diet-induced obesity.References1. Chang, M.R., Ciesla, A., Strutzenberg, T.S., et al. Unique polypharmacology nuclear receptor modulator blocks inflammatory signaling pathways. ACS Chem. Biol. 14(5), 1051-1062 (2019). SR 1903 is a modulator of retinoic acid receptor-related orphan receptor γ (RORγ) and liver X receptor (LXR).1 It is an inverse agonist of RORγ (IC50 = ~100 nM in a cell-based reporter assay) and an agonist of LXR. It also binds to peroxisome proliferator-activated receptor γ (PPARγ; IC50 = 209 nM) but does not activate it. SR 1903 (10 μM) inhibits LPS-induced expression of triggering receptor expressed on myeloid cells 1 (TREM-1) in RAW 264.7 cells. It also inhibits LPS-induced expression of the LXR target genes IL-6 and IL-33 and increases expression of ABCG1, FASN, and SCD-1 in RAW 264.7 cells. SR 1903 (20 mg/kg twice per day) reduces severity score in a mouse model of collagen-induced arthritis. It reduces blood glucose levels in a glucose tolerance test, serum levels of total cholesterol and LDL, body weight, and fat mass in a mouse model of high-fat diet-induced obesity. References1. Chang, M.R., Ciesla, A., Strutzenberg, T.S., et al. Unique polypharmacology nuclear receptor modulator blocks inflammatory signaling pathways. ACS Chem. Biol. 14(5), 1051-1062 (2019).

5-Hydroxy Lansoprazole Sulfide is an inhibitor of fatty acid synthase (FASN). FASN, which is responsible for de-novo synthesis of lipids, has been found to be overexpressed in cancerous tissue. 5-Hydroxy Lansoprazole Sulfide specifically inhibits enoyl reductase, and was found to more effectively inhibit FASN function than lansoprazole and was also more efficient at regulating NHEJ repair of oxidative DNA damage via PARP1.

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 (IC50: 7.13 μM).

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.

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).

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.

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.

Podocarpusflavone A is a DNA topoisomerase I and STAT3 inhibitor, a flavonoid chemically inactive isolated from the endemic Taiwanese plant, Luo Han Guo, with potential antileishmanial activity and antitumor activity.Podocarpusflavone A, inhibits the cell growth of cutaneous dermal melanoma.

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