Fatty Acid Synthase

Fatty Acid Synthase製品

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  • Fatty Acid Synthase阻害剤 (18)
  • Fatty Acid Synthase活性剤(1)
  • Fatty Acid Synthaseモジュレータ(1)
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S2697 A-769662 A-769662 is a potent, reversible AMPK activator with EC50 of 0.8 μM in cell-free assays, little effect on GPPase/FBPase activity.
J Clin Invest, 2024, 134(22)e181314
Nat Commun, 2023, 14(1):5913
Nat Commun, 2023, 14(1):5913
S2250 EGCG ((-)-Epigallocatechin Gallate) EGCG ((-)-Epigallocatechin Gallate) is the main catechin extraction of green tea that inhibits telomerase and DNA methyltransferase. EGCG blocks the activation of EGF receptors and HER-2 receptors. ECGG inhibits fatty acid synthase and glutamate dehydrogenase activity.
Journal of Functional Foods, 2024, 105977
Cell Rep Med, 2023, 4(5):101026
Transl Oncol, 2023, 35:101712
S1629 Orlistat Orlistat is a general lipase inhibitor with IC50 of 122 ng/ml for PL from human duodenal juice. Orlistat treatment reduces proliferation, induces apoptosis and arrests cell cycle.
J Cell Sci, 2024, 137(20)jcs262162
iScience, 2023, 26(3):106193
iScience, 2023, 26(3):106193
S8284 Fatostatin HBr Fatostatin HBr is an inhibitor of sterol regulatory element binding protein (SREBP). It impairs the activation of SREBP-1 and SREBP-2.
Cell Rep, 2023, 42(8):112963
Respir Res, 2023, 24(1):8
Ann Transl Med, 2022, 10(18):958
S9714 Denifanstat (TVB-2640) Denifanstat (TVB-2640) is an orally bioavailable, pharmacological fatty acid synthase (FAS/FASN) inhibitor with therapeutic potential in patients with NAFLD and nonalcoholic steatohepatitis.
Nat Genet, 2024, 10.1038/s41588-024-01891-8
Cell Rep, 2023, 42(9):113034
J Transl Med, 2023, 21(1):32
S1937 Isoniazid Isoniazid is a prodrug that blocks the action of fatty acid synthase by interacting with KatG , used for the prevention and treatment of tuberculosis.
mBio, 2022, e0302422.
Nat Metab, 2021, 10.1038/s42255-021-00479-4
Front Immunol, 2021, 12:712021
S4754 Betulin Betulin (BE, betulinol, betuline, betulinic alcohol), also known as betulinol, betuline, or betulinic alcohol, is a pentacyclic lupane-type triterpenoid naturally distributed in many plants and displays a broad spectrum of biological and pharmacological properties such as anticancer and chemopreventive activity.
Acta Biochim Biophys Sin -Shanghai), 2023, 55(9):1479-1486
Acta Biochim Biophys Sin (Shanghai), 2023, 55(9):1479-1486
Nat Metab, 2021, 10.1038/s42255-021-00479-4
S8563 TVB-3664 TVB-3664 is a potent, selective, orally active and reversible inhibitor of fatty acid synthase (FASN) with IC50 of 0.018 μM and 0.012 μM for human and mouse cell palmitate synthesis, respectively.
Nat Commun, 2023, 14(1):1362
bioRxiv, 2023, 2023.07.05.547848
bioRxiv, 2023, 2023.07.05.547848
S6666 FT113 FT113 is a potent inhibitor of fatty acid synthase (FAS/FASN) with ic50 of 213 nM.
Nat Cancer, 2023, 4(10):1508-1525
Nat Cancer, 2023, 10.1038/s43018-023-00635-7
Nat Metab, 2021, 10.1038/s42255-021-00479-4
S9785 Fatostatin

Fatostatin (125B11), a diarylthiazole derivative, is a specific inhibitor of Sterol regulatory element binding proteins (SREBPs) activation. Fatostatin binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs. Fatostatin suppresses growth and enhances apoptosis in cancer cells.

Oncogene, 2024, 43(4):281-293
Biochem Pharmacol, 2024, 224:116207
bioRxiv, 2024, 10.1101/2024.01.16.575899
S8915 C75 trans C75 trans (trans-C75, (±)-C75) is a novel, potent synthetic inhibitor of fatty acid synthase (FAS/FASN) with IC50 of 35 μM and 50 μM in clonogenic assays and spheroid growth assay, respectively. C75 is used as a tool for studying fatty acid synthesis in metabolic disorders and cancer.
Signal Transduct Target Ther, 2022, 7(1):46
Nat Metab, 2021, 10.1038/s42255-021-00479-4
S3300 Desoxyrhaponticin Desoxyrhaponticin (DC, DES), a stilbene glycoside from Rheum tanguticum Maxim. ex Balf. (rhubarb) which is a traditional Chinese nutritional food, is a fatty acid synthase (FAS/FASN) inhibitor. Desoxyrhaponticin (DC, DES) is also a competitive inhibitor of glucose uptake with IC50 of 148.3 μM and 30.9 μM in rabbit intestinal membrane vesicles and in rat everted gut sleeves, respectively. Desoxyrhaponticin has apoptotic effect on human cancer cells.
Nat Metab, 2021, 10.1038/s42255-021-00479-4
E2641 trans-Chalcone Trans-Chalcone, the backbone of flavonoids, also is a potent fatty acid synthase (FAS) with IC50 of 17.1 μg/mL, and α-amylase inhibitor, causes cellcycle arrest and induces apoptosis in the breastcancer cell line MCF-7, exerting antifungal and anticancer activities.
E2667 IPI-9119 IPI-9119 is a potent, selective, and irreversible inhibitor of fatty acid synthase (FASN), which can inhibit the FASN thioesterase domain by promoting acylation of the catalytic serine with an IC50 of 0.3 nM.
S6466 Eicosapentaenoic acid ethyl ester Eicosapentaenoic acid ethyl ester (AMR101, EPA ethyl ester, Ethyl eicosapentaenoate) is an omega-3 fatty acid agent that significantly reduces the triglyceride (TG) levels and improves other lipid parameters without significantly increasing the low-density lipoprotein (LDL) cholesterol levels.
E2900 Sodium palmitate Sodium palmitate(Palmitic acid sodium) is a common saturated fatty acid and produced during fatty acid synthesis. Sodium palmitate enhances lipogenesis and cellular steatosis in various cell lines.
Cancer Lett, 2024, 597:217068
S2314 Kaempferol Kaempferol, a natural flavonol, functions as an ERRα and ERRγ inverse agonist. It inhibits topoisomerase I catalyzed DNA religation and may also inhibit the activity of fatty acid synthase.
Int J Mol Sci, 2023, 24(19)14519
Front Pharmacol, 2023, 14:1047184
Front Pharmacol, 2023, 14:1047184
S3576 TVB-3166 TVB-3166 is an orally-available, reversible, potent and selective inhibitor of fatty acid synthase (FASN) with IC50 of 0.042 μM in an in vitro biochemical assay. TVB-3166 induces apoptosis, and inhibits in-vivo xenograft tumor growth.
S9392 Praeruptorin B Praeruptorin B is an important compound isolated from Bai-hua Qian-hu and has been reported to exert multiple biochemical and pharmacological activities.
Nat Metab, 2021, 10.1038/s42255-021-00479-4
S6248 Fasnall Fasnall, a thiophenopyrimidine, is a selective fatty acid synthase (FASN) inhibitor that shows potent anti-tumor activity.
S2697 A-769662 A-769662 is a potent, reversible AMPK activator with EC50 of 0.8 μM in cell-free assays, little effect on GPPase/FBPase activity.
J Clin Invest, 2024, 134(22)e181314
Nat Commun, 2023, 14(1):5913
Nat Commun, 2023, 14(1):5913
S2250 EGCG ((-)-Epigallocatechin Gallate) EGCG ((-)-Epigallocatechin Gallate) is the main catechin extraction of green tea that inhibits telomerase and DNA methyltransferase. EGCG blocks the activation of EGF receptors and HER-2 receptors. ECGG inhibits fatty acid synthase and glutamate dehydrogenase activity.
Journal of Functional Foods, 2024, 105977
Cell Rep Med, 2023, 4(5):101026
Transl Oncol, 2023, 35:101712
S1629 Orlistat Orlistat is a general lipase inhibitor with IC50 of 122 ng/ml for PL from human duodenal juice. Orlistat treatment reduces proliferation, induces apoptosis and arrests cell cycle.
J Cell Sci, 2024, 137(20)jcs262162
iScience, 2023, 26(3):106193
iScience, 2023, 26(3):106193
S8284 Fatostatin HBr Fatostatin HBr is an inhibitor of sterol regulatory element binding protein (SREBP). It impairs the activation of SREBP-1 and SREBP-2.
Cell Rep, 2023, 42(8):112963
Respir Res, 2023, 24(1):8
Ann Transl Med, 2022, 10(18):958
S9714 Denifanstat (TVB-2640) Denifanstat (TVB-2640) is an orally bioavailable, pharmacological fatty acid synthase (FAS/FASN) inhibitor with therapeutic potential in patients with NAFLD and nonalcoholic steatohepatitis.
Nat Genet, 2024, 10.1038/s41588-024-01891-8
Cell Rep, 2023, 42(9):113034
J Transl Med, 2023, 21(1):32
S1937 Isoniazid Isoniazid is a prodrug that blocks the action of fatty acid synthase by interacting with KatG , used for the prevention and treatment of tuberculosis.
mBio, 2022, e0302422.
Nat Metab, 2021, 10.1038/s42255-021-00479-4
Front Immunol, 2021, 12:712021
S4754 Betulin Betulin (BE, betulinol, betuline, betulinic alcohol), also known as betulinol, betuline, or betulinic alcohol, is a pentacyclic lupane-type triterpenoid naturally distributed in many plants and displays a broad spectrum of biological and pharmacological properties such as anticancer and chemopreventive activity.
Acta Biochim Biophys Sin -Shanghai), 2023, 55(9):1479-1486
Acta Biochim Biophys Sin (Shanghai), 2023, 55(9):1479-1486
Nat Metab, 2021, 10.1038/s42255-021-00479-4
S8563 TVB-3664 TVB-3664 is a potent, selective, orally active and reversible inhibitor of fatty acid synthase (FASN) with IC50 of 0.018 μM and 0.012 μM for human and mouse cell palmitate synthesis, respectively.
Nat Commun, 2023, 14(1):1362
bioRxiv, 2023, 2023.07.05.547848
bioRxiv, 2023, 2023.07.05.547848
S6666 FT113 FT113 is a potent inhibitor of fatty acid synthase (FAS/FASN) with ic50 of 213 nM.
Nat Cancer, 2023, 4(10):1508-1525
Nat Cancer, 2023, 10.1038/s43018-023-00635-7
Nat Metab, 2021, 10.1038/s42255-021-00479-4
S9785 Fatostatin

Fatostatin (125B11), a diarylthiazole derivative, is a specific inhibitor of Sterol regulatory element binding proteins (SREBPs) activation. Fatostatin binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs. Fatostatin suppresses growth and enhances apoptosis in cancer cells.

Oncogene, 2024, 43(4):281-293
Biochem Pharmacol, 2024, 224:116207
bioRxiv, 2024, 10.1101/2024.01.16.575899
S8915 C75 trans C75 trans (trans-C75, (±)-C75) is a novel, potent synthetic inhibitor of fatty acid synthase (FAS/FASN) with IC50 of 35 μM and 50 μM in clonogenic assays and spheroid growth assay, respectively. C75 is used as a tool for studying fatty acid synthesis in metabolic disorders and cancer.
Signal Transduct Target Ther, 2022, 7(1):46
Nat Metab, 2021, 10.1038/s42255-021-00479-4
S3300 Desoxyrhaponticin Desoxyrhaponticin (DC, DES), a stilbene glycoside from Rheum tanguticum Maxim. ex Balf. (rhubarb) which is a traditional Chinese nutritional food, is a fatty acid synthase (FAS/FASN) inhibitor. Desoxyrhaponticin (DC, DES) is also a competitive inhibitor of glucose uptake with IC50 of 148.3 μM and 30.9 μM in rabbit intestinal membrane vesicles and in rat everted gut sleeves, respectively. Desoxyrhaponticin has apoptotic effect on human cancer cells.
Nat Metab, 2021, 10.1038/s42255-021-00479-4
E2641 trans-Chalcone Trans-Chalcone, the backbone of flavonoids, also is a potent fatty acid synthase (FAS) with IC50 of 17.1 μg/mL, and α-amylase inhibitor, causes cellcycle arrest and induces apoptosis in the breastcancer cell line MCF-7, exerting antifungal and anticancer activities.
E2667 IPI-9119 IPI-9119 is a potent, selective, and irreversible inhibitor of fatty acid synthase (FASN), which can inhibit the FASN thioesterase domain by promoting acylation of the catalytic serine with an IC50 of 0.3 nM.
S2314 Kaempferol Kaempferol, a natural flavonol, functions as an ERRα and ERRγ inverse agonist. It inhibits topoisomerase I catalyzed DNA religation and may also inhibit the activity of fatty acid synthase.
Int J Mol Sci, 2023, 24(19)14519
Front Pharmacol, 2023, 14:1047184
Front Pharmacol, 2023, 14:1047184
S3576 TVB-3166 TVB-3166 is an orally-available, reversible, potent and selective inhibitor of fatty acid synthase (FASN) with IC50 of 0.042 μM in an in vitro biochemical assay. TVB-3166 induces apoptosis, and inhibits in-vivo xenograft tumor growth.
S9392 Praeruptorin B Praeruptorin B is an important compound isolated from Bai-hua Qian-hu and has been reported to exert multiple biochemical and pharmacological activities.
Nat Metab, 2021, 10.1038/s42255-021-00479-4
S6248 Fasnall Fasnall, a thiophenopyrimidine, is a selective fatty acid synthase (FASN) inhibitor that shows potent anti-tumor activity.
E2900 Sodium palmitate Sodium palmitate(Palmitic acid sodium) is a common saturated fatty acid and produced during fatty acid synthesis. Sodium palmitate enhances lipogenesis and cellular steatosis in various cell lines.
Cancer Lett, 2024, 597:217068
S6466 Eicosapentaenoic acid ethyl ester Eicosapentaenoic acid ethyl ester (AMR101, EPA ethyl ester, Ethyl eicosapentaenoate) is an omega-3 fatty acid agent that significantly reduces the triglyceride (TG) levels and improves other lipid parameters without significantly increasing the low-density lipoprotein (LDL) cholesterol levels.

Fatty Acid Synthase阻害剤の選択性比較

Tags: FASN inhibition | FASN activation | FASN activity | FASN inhibitors in clinical trials | FASN inhibitor review