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. |
-
Nat Commun, 2023, 14(1):5913
-
Nat Commun, 2023, 14(1):5913
-
J Adv Res, 2023, 43:13-26
|
|
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. |
-
iScience, 2023, 26(3):106193
-
iScience, 2023, 26(3):106193
-
OPARU, 2023, 10.18725/OPARU-48911
|
|
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. Betulin (Trochol), is a sterol regulatory element-binding protein (SREBP) inhibitor with an IC50 of 14.5 μM in K562 cell line. |
-
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
-
EMBO J, 2022, e109463
|
|
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.praeruptorin B exerts lipid-lowering effects through inhibits SREBPs and could serve as a possible therapeutic option to improve hyperlipidemia and hyperlipidemia-induced comorbidities. |
-
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. |
- Nat Commun, 2023, 14(1):5913
- Nat Commun, 2023, 14(1):5913
- J Adv Res, 2023, 43:13-26
|
|
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. |
- iScience, 2023, 26(3):106193
- iScience, 2023, 26(3):106193
- OPARU, 2023, 10.18725/OPARU-48911
|
|
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. Betulin (Trochol), is a sterol regulatory element-binding protein (SREBP) inhibitor with an IC50 of 14.5 μM in K562 cell line. |
- 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
- EMBO J, 2022, e109463
|
|
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.praeruptorin B exerts lipid-lowering effects through inhibits SREBPs and could serve as a possible therapeutic option to improve hyperlipidemia and hyperlipidemia-induced comorbidities. |
- 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. |
|
|