Fatty Acid Synthase (FASN) Inhibitor

Fasnall is a selective fatty acid synthase (FASN) inhibitor with an IC₅₀ of 3.71 μM. Fasnall induces apoptosis in HER2⁺ breast cancer cell lines. Fasnall shows potent anti-tumor activities.

Xelafaslatide (ONL-1204) is a Fas receptor antagonist. Xelafaslatide blocks the Fas receptor signaling pathway and inhibits downstream apoptosis and inflammatory pathways. Xelafaslatide suppresses neuroinflammation and microglial activation in glaucoma models, protects retinal ganglion cells and prevents axonal degeneration. Xelafaslatide is applicable to relevant research on glaucoma.

Ginkgolic acid C17:1 is a fatty acid synthase (FAS) inhibitor with an IC₅₀ of 10.5 µM. Ginkgolic acid C17:1 shows anti-tumor activity by inhibiting the phosphorylation of STAT3 and inducing apoptosis. Ginkgolic acid C17:1 can block the interaction between S-RBD and ACE2, and has anti-SARS-CoV-2-S pseudovirus activity. Ginkgolic acid C17:1 inhibits the biofilm formation of enterohemorrhagic Escherichia coli and Staphylococcus aureus.

Pseudoprotodioscin, a furostanoside, inhibits SREBP1/2 and microRNA 33a/b levels and reduces the gene expression regarding the synthesis of cholesterol and triglycerides.

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

Clitorin is an orally active flavonoid compound that can be isolated from Carica papaya. Clitorin is an inhibitor of EGFR (IC₅₀: 89.58 nM) and aromatase (IC₅₀: 77.41 nM). Clitorin has antioxidant and anti-tumor activities. In the DPPH and ABTS radical scavenging assays, Clitorin has IC₅₀ values of 91.96 ppm and 250.45 ppm, respectively. In addition, Clitorin can regulate lipogenesis and fatty acid oxidation and can be used in the research of non-alcoholic fatty liver disease.

trans-Chalcone, isolated from Aronia melanocarpa skin, is a biphenolic core structure of flavonoids precursor. trans-Chalcone is a potent fatty acid synthase (FAS) and α-amylase inhibitor. trans-Chalcone causes cellcycle arrest and induces apoptosis in the breastcancer cell line MCF-7. trans-Chalcone has antifungal and anticancer activity.

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. In cell-based assay, FT113 blocks FASN activity in BT474 cells (IC₅₀, 90 nM). FT113 shows anti-proliferative activity, and exhibits anti-cancer activity both in vitro and in vivo.

Yamogenin (Neodiosgenin) is a diastereomer of diosgenin. Yamogenin antagonizes the activation of the liver X receptor (LXR) in luciferase ligand assay. Yamogenin inhibits triacylglyceride (TG) accumulation through the suppression of gene expression of fatty acid synthesis in HepG2 hepatocytes. Yamogenin is a steroidal saponin that can be obtained from plant species with in vitro cytotoxicity, antioxidant, and antimicrobial properties. Yamogenin induces cell death via the extrinsic and intrinsic way of apoptosis. Yamogenin inhibits protein denaturation with an IC₅₀ of 1421.92 μg/mL. Yamogenin can be studied in research on gastric cancer.

Thiolactomycin is an orally active bacterial type II fatty acid synthase (FAS-II) inhibitor with antibacterial and antimalarial activities. Thiolactomycin specifically targets KasA/KasB in mycobacteria and FabB/FabF in bacteria, thereby inhibiting the biosynthesis of fatty acids and mycolic acids. Thiolactomycin can be used in studies related to tuberculosis, systemic bacterial infections, and experimental pyelonephritis.

Maltitol is an orally active polyol and sugar alcohol sweetener produced by the hydrogenation of maltose. Maltitol can replace sucrose and has characteristics of having a minor impact on blood sugar and potential prebiotic effects.

Desoxyrhaponticin is a kind of oral drug that inhibits effective fatty acid synthesis (FASN), and has a fatal effect on cancer cells. Desoxyrhaponticin has the ability to inhibit glucose uptake, improve oral glucose tolerance as a diabetic agent, and possess anti-diabetic effects.

Prothioconazole is an orally active broad-spectrum fungicide. Prothioconazole weakly inhibits CaCYP51 activity in Candida albicans, with an apparent IC₅₀ of approximately 120 μM. Prothioconazole disrupts Microtubule stability by reducing the acetylation level of α-tubulin. Prothioconazole induces Mitochondrial dysfunction, oxidative stress, DNA damage, and Apoptosis. Prothioconazole accumulates ¹⁴-methylated sterols and depletes ergosterol in cells, culture media, plants, and animals. Prothioconazole interferes with pyruvate metabolism and glycolysis/gluconeogenesis processes in mouse liver, downregulates Fasn mRNA expression, and induces hepatotoxicity and renal metabolic disorders. Prothioconazole reduces the fertility of female mice. Prothioconazole inhibits body weight gain and increases liver/kidney indices in mice. Prothioconazole can be used in studies related to candidiasis.

FASN-IN-4 tosylate is a potent inhibitor of fatty acid synthase (FASN) with an IC₅₀ of 10 nM (WO2012064642A1, compound 29). FASN-IN-4 tosylate also inhibits SARS-CoV-2 with an EC₅₀ of 18.6?nM.

UCM05 (G28UCM) is a fatty acid synthase (FASN) and filamentous temperature-sensitive protein Z (Ftsz) inhibitor. UCM05 inhibits fatty acid synthesis, viral replication, and Gram-positive bacterial growth. UCM05 binds to FtsZ GTP-binding sites, inhibits GTPase activity, and disrupts Z-ring localization. UCM05 can be used for the research of HSV-1/2 infection, HIV-1 infection, and Gram-positive bacterial infections^[1][2][3].

Desoxyrhaponticin (Standard) is the analytical standard of Desoxyrhaponticin. This product is intended for research and analytical applications. Desoxyrhaponticin is a kind of oral drug that inhibits effective fatty acid synthesis (FASN), and has a fatal effect on cancer cells. Desoxyrhaponticin has the ability to inhibit glucose uptake, improve oral glucose tolerance as a diabetic agent, and possess anti-diabetic effects.

PF429242 is a reversible and competitive SREBP site 1 protease (S1P) inhibitor with an IC₅₀ of 175 nM.

FASN-IN-1 is a fatty acid synthase (FASN) inhibitor extracted from patent WO2015134790A1, compound 56.

Alisol A 24-acetate (Alisol A monoacetate) is an orally active derivative of protostane-type tetracyclic triterpenoid. Alisol A 24-acetate upregulates the expression of adiponectin, AMPKα, CPT1, and ACOX1; downregulates the expression of SREBP-1c, ACC, FAS, Bcl-2, Bcl-xl, PPAR-γ, perilipin A, and NFATc1; inhibits the activity of PI3K/Akt/mTOR and HMGR; and activates the PKA and ERK signaling pathways. Alisol A 24-acetate regulates cell apoptosis (apoptosis), autophagy (Autophagy, hepatic lipid accumulation, inflammatory response, neuroprotection, MRSA membrane integrity, and osteoclast differentiation. Alisol A 24-acetate can be used in research related to non-alcoholic fatty liver disease, nephrotoxicity, obesity, global cerebral ischemia-reperfusion injury, bacterial infection, and osteoporosis.

Nicodicosapent is a fatty acid niacin conjugate that is also an inhibitor of the sterol regulatory element binding protein (SREBP), a key regulator of cholesterol metabolism proteins such as PCSK9, HMG-CoA reductase, ATP citrate lyase, and NPC1L1.