Fatty-Acid-Synthase-FASN-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Fatty Acid Synthase (FAS).html Fatty HYPERLINK https:/www.MedChemE/Targets/Fatty Acid Synthase (FAS).html HYPERLINK https:/www.MedChemE/Targets/Fatty Acid Synthase (FAS).html Acid HYPERLINK https:/www.MedChemE/Targets/Fatty Acid Synthase (FAS).html HYPERLINK ht

2、tps:/www.MedChemE/Targets/Fatty Acid Synthase (FAS).html Synthase HYPERLINK https:/www.MedChemE/Targets/Fatty Acid Synthase (FAS).html HYPERLINK https:/www.MedChemE/Targets/Fatty Acid Synthase (FAS).html (FASN)Fatty Acid Synthase (FASN) is a multifunctional homodimeric enzyme protein, and it is the

3、major enzyme required for the anabolicconversion of dietary carbohydrates to fatty acids. Fatty acid synthase catalyzes the conversion of acetyl-CoA and malonyl-CoA, inthe presence of NADPH, into long-chain saturated fatty acids.Human fatty acid synthase is a large homodimeric multifunctional enzyme

4、 that synthesizes palmitic acid. The unique carboxylterminal thioesterase domain of fatty acid synthase hydrolyzes the growing fatty acid chain and plays a critical role in regulating thechain length of fatty acid released. Also, the up-regulation of human fatty acid synthase in a variety of cancer

5、makes thethioesterase a candidate target for therapeutic treatment.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/Fatty Acid Synthase (FAS).html Fatty HYPERLINK https:/www.MedChemE/Targets/Fatty Acid Synthase (FAS).html HYPERLINK https:/www.MedChemE/Targets/Fatty Acid Synthase (FAS).html Acid

6、HYPERLINK https:/www.MedChemE/Targets/Fatty Acid Synthase (FAS).html HYPERLINK https:/www.MedChemE/Targets/Fatty Acid Synthase (FAS).html Synthase HYPERLINK https:/www.MedChemE/Targets/Fatty Acid Synthase (FAS).html HYPERLINK https:/www.MedChemE/Targets/Fatty Acid Synthase (FAS).html (FASN) HYPERLIN

7、K https:/www.MedChemE/Targets/Fatty Acid Synthase (FAS).html HYPERLINK https:/www.MedChemE/Targets/Fatty Acid Synthase (FAS).html Inhibitors HYPERLINK https:/www.MedChemE/Targets/Fatty Acid Synthase (FAS).html HYPERLINK https:/www.MedChemE/Targets/Fatty Acid Synthase (FAS).html & HYPERLINK https:/ww

8、w.MedChemE/Targets/Fatty Acid Synthase (FAS).html HYPERLINK https:/www.MedChemE/Targets/Fatty Acid Synthase (FAS).html Modulators HYPERLINK https:/www.MedChemE/albaspidin-ap.html Albaspidin HYPERLINK https:/www.MedChemE/albaspidin-ap.html HYPERLINK https:/www.MedChemE/albaspidin-ap.html APCat. No.:

9、HY-N0200 HYPERLINK https:/www.MedChemE/Betulin.html Betulin(Trochol) Cat. No.: HY-N0083Albaspidin AP inhibits fatty acid synthase (FAS)with an IC value of 71.7 M. Fatty acid synthase50(FAS) is emerging as a potential therapeutictarget for cancer and obesity.Betulin (Trochol), is a sterol regulatorye

10、lement-binding protein (SREBP) inhibitor with anIC of 14.5 M in K562 cell line.50Purity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mgPurity: 98.0%Clinical Data: No Development ReportedSize: 50 mg, 100 mg, 200 mg HYPERLINK https:/www.MedChemE/bi99179.html BI HYPERLINK https:/www.

11、MedChemE/bi99179.html HYPERLINK https:/www.MedChemE/bi99179.html 99179 HYPERLINK https:/www.MedChemE/bi99179.html HYPERLINK https:/www.MedChemE/C75.html C75Cat. No.: HY-16100 Cat. No.: HY-12364BI 99179 is a potent and selective type I fattyacid synthase (FAS) inhibitor with an IC of 7950nM. BI 99179

12、 is a tool compound suitable for thein vivo validation of FAS as a target for lipidmetabolism related diseases.C75 is a synthetic fatty-acid synthase (FASN)inhibitor; inhibits prostate cancer cells PC3 withan IC50 of 35 M. C75 is a potent CPT1Aactivator.Purity: 99.78%Clinical Data: No Development Re

13、portedSize: 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.91%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/Cerulenin.html CeruleninCat. No.: HY-A0210 HYPERLINK https:/www.MedChemE/fasn-in-2.html Denifanstat(TVB-2640; FASN-IN-2; ASC-40) Cat. No.: HY-1

14、12829Cerulenin, a potent, natural inhibitor of fattyacid synthase (FASN), is an epoxide produced bythe fungus Cephalosporium caeruleus. Cerulenininhibits topoisomerase I catalytic activity andaugments SN-38-induced apoptosis. Cerulenin hasantifungal and antitumor activies.Denifanstat (TVB-2640) is a

15、n orally active andpotent Fatty Acid Synthase (FASN) inhibitor withan IC50 of 0.052 M and an EC50 of 0.072 M.Denifanstat has the potential for fatty liverdisease and cancer research.Purity: 98.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mgPurity: 99.69%Clinical Data: Phase 2Size: 10

16、mM 1 mL, 5 mg, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/desoxyrhaponticin.html Desoxyrhaponticin HYPERLINK https:/www.MedChemE/desoxyrhaponticin.html HYPERLINK https:/www.MedChemE/dihydrocurcumin.html DihydrocurcuminCat. No.: HY-N2486 Cat. No.: HY-N1967Desoxyrhaponticin is a stilbene glycoside fro

17、m theTibetan nutritional food Rheum tanguticumMaxim. Desoxyrhaponticin is a Fatty acid synthase(FASN) inhibitor, and has apoptotic effect onhuman cancer cells.Dihydrocurcumin, a major metabolites of curcumin,reduces lipid accumulation and oxidative stress.Purity: 99.80%Clinical Data: No Development

18、ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mgPurity: 99.77%Clinical Data: No Development ReportedSize: 5 mg, 10 mg HYPERLINK https:/www.MedChemE/fasn-in-1.html FASN-IN-1 HYPERLINK https:/www.MedChemE/fasn-in-1.html HYPERLINK https:/www.MedChemE/Heterocyclic_modulators_1.html FASN-IN-3Cat. No.: HY-111

19、777 Cat. No.: HY-U00436FASN-IN-1 is a fatty acid synthase (FASN)inhibitor extracted from patent WO2015134790A1,compound 56.FASN-IN-3 is a fatty acid synthase (FASN)inhibitor extracted from patent US20170119786A1,compound 242A.Purity: 99.62%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg

20、, 10 mg, 50 mg, 100 mgPurity: 98.17%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/FAS-IN-1.html FASN-IN-4 HYPERLINK https:/www.MedChemE/FAS-IN-1.html HYPERLINK https:/w

21、ww.MedChemE/FAS-IN-1-Tosylate.html FASN-IN-4 HYPERLINK https:/www.MedChemE/FAS-IN-1-Tosylate.html HYPERLINK https:/www.MedChemE/FAS-IN-1-Tosylate.html tosylateCat. No.: HY-12648 Cat. No.: HY-12648AFASN-IN-4 is a potent inhibitor of fatty acidsynthase (FASN) with an IC of 10 nM50(WO2012064642A1, comp

22、ound 29). FASN-IN-4 alsoinhibits SARS-CoV-2 with an EC of 18.6nM.50FASN-IN-4 tosylate is a potent inhibitor of fattyacid synthase (FASN) with an IC of 10 nM50(WO2012064642A1, compound 29). FASN-IN-4 tosylatealso inhibits SARS-CoV-2 with an EC of5018.6nM.Purity: 99.21%Clinical Data: No Development Re

23、portedSize: 10 mM 1 mL, 2 mgPurity: 98.63%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 2 mg, 5 mg, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/fasn-in-5.html FASN-IN-5Cat. No.: HY-145809 HYPERLINK https:/www.MedChemE/Fatostatin-A.html Fatostatin(125B11) Cat. No.: HY-14452FASN-IN-5 (example

24、 11), a FASN inhibitor, can beused for the research of TH17- or CSF1 -mediateddisease or disorder such as cancer, immunologicaldisorders, and obesity.Fatostatin (125B11), a specific inhibitor ofSREBP activation, impairs the activation ofSREBP-1 and SREBP-2. Fatostatin binds to SCAP(SREBP cleavage-ac

25、tivating protein), and inhibitsthe ER-Golgi translocation of SREBPs.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.20%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/fatostatin-hydrobromide.html Fato

26、statin HYPERLINK https:/www.MedChemE/fatostatin-hydrobromide.html HYPERLINK https:/www.MedChemE/fatostatin-hydrobromide.html hydrobromide(125B11 hydrobromide) Cat. No.: HY-14452A HYPERLINK https:/www.MedChemE/FGH10019.html FGH10019Cat. No.: HY-16207Fatostatin hydrobromide (125B11 hydrobromide), aspe

27、cific inhibitor of SREBP activation, impairsthe activation of SREBP-1 and SREBP-2. Fatostatinhydrobromide binds to SCAP (SREBPcleavage-activating protein), and inhibits theER-Golgi translocation of SREBPs.FGH10019 is a novel sterol regulatoryelement-binding protein (SREBP) inhibitor withIC of 1 M.50

28、Purity: 99.61%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.43%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/FT113.html FT113 HYPERLINK https:/www.MedChemE/FT113.html HYPERLINK https:/www

29、.MedChemE/HS79.html HS79Cat. No.: HY-111551 Cat. No.: HY-112522FT113 is a potent and orally active fatty acidsynthase (FASN) inhibitor, with an IC of 213 nM50for full-length recombinant human FASN enzyme. Incell-based assay, FT113 blocks FASN activity inBT474 cells (IC , 90 nM).50HS-79 is an enantio

30、mer of Fasnall, which is aselective fatty acid synthase (FASN) inhibitor.HS-79 is able to inhibit the incorporation oftritiated acetate into lipids with an IC of 1.5750M.Purity: 99.61%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Devel

31、opment ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/HS80.html HS80 HYPERLINK https:/www.MedChemE/HS80.html HYPERLINK https:/www.MedChemE/ipi-9119.html IPI-9119Cat. No.: HY-112522A Cat. No.: HY-124628HS-80 is an enantiomer of Fasnall, which is aselective fatty acid synthase (FASN) inhibitor

32、.HS-80 is able to inhibit the incorporation oftritiated acetate into lipids with an IC of 7.1350M.IPI-9119 is an orally active, selective andirreversible FASN inhibitor with an IC of 0.350nM in vitro biochemical assay. IPI-9119 inhibitstumor growth of castration-resistant prostatecancer (CRPC) xenog

33、rafts mouse models.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.13%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/leelamine-hydrochloride.html Leelamine HYPERLINK https:/www.MedChemE

34、/leelamine-hydrochloride.html HYPERLINK https:/www.MedChemE/leelamine-hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/leelamine-hydrochloride.html HYPERLINK https:/www.MedChemE/leelamine-d4-hydrochloride.html Leelamine-d4 HYPERLINK https:/www.MedChemE/leelamine-d4-hydrochloride.html H

35、YPERLINK https:/www.MedChemE/leelamine-d4-hydrochloride.html hydrochlorideCat. No.: HY-110028 Cat. No.: HY-110028SLeelamine hydrochloride is a tricyclic diterpenemolecule that is extracted from the bark of pinetrees.Leelamine-d4 hydrochloride is the deuteriumlabeled Leelamine hydrochloride. Leelamin

36、ehydrochloride is a tricyclic diterpene moleculethat is extracted from the bark of pine trees.Purity: 98%Clinical Data:Size: 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/lycorine.html Lycorine HYPERLINK https:/www.MedChemE/lycorine.html HYPERLIN

37、K https:/www.MedChemE/Nicodicosapent.html NicodicosapentCat. No.: HY-N0288 Cat. No.: HY-17640Lycorine is a natural alkaloid extracted from theAmaryllidaceae plant. Lycorine is a potent andorally active SCAP inhibitor with a K valued15.24 nM. Lycorine downregulates the SCAP proteinlevel without chang

38、ing its transcription.Nicodicosapent is a fatty acid niacin conjugatethat is also an inhibitor of the sterol regulatoryelement binding protein (SREBP), a key regulatorof cholesterol metabolism proteins such as PCSK9,HMG-CoA reductase, ATP citrate lyase, and NPC1L1.Purity: 98.0%Clinical Data: No Deve

39、lopment ReportedSize: 50 mg, 100 mgPurity: 98.04%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 2 mg, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/orlistat.html Orlistat(Tetrahydrolipstatin; Ro-18-0647) Cat. No.: HY-B0218 HYPERLINK https:/www.MedChemE/pedunculoside.html Peduncul

40、osideCat. No.: HY-N0458Orlistat (Tetrahydrolipstatin) is a well-knownirreversible inhibitor of pancreatic and gastriclipases. Orlistat is also an inhibitor of fattyacid synthase (FASN), is used orally forlong-term research ofobesity. Anti-atherosclerotic effect.Pedunculoside exerts lipid-lowering ef

41、fects partlythrough the regulationof lipogenesis and fatty acid-oxidation.Purity: 98.88%Clinical Data: LaunchedSize: 10 mM 1 mL, 100 mg, 200 mg, 500 mgPurity: 99.17%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 20 mg HYPERLINK https:/www.MedChemE/PF429242_dihydrochloride.html PF429242 HYP

42、ERLINK https:/www.MedChemE/PF429242_dihydrochloride.html HYPERLINK https:/www.MedChemE/PF429242_dihydrochloride.html dihydrochloride HYPERLINK https:/www.MedChemE/PF429242_dihydrochloride.html HYPERLINK https:/www.MedChemE/Praeruptorin_B.html Praeruptorin HYPERLINK https:/www.MedChemE/Praeruptorin_B

43、.html HYPERLINK https:/www.MedChemE/Praeruptorin_B.html BCat. No.: HY-13447A(Praeruptorin D) Cat. No.: HY-N0082PF429242 dihydrochloride is a reversible andcompetitive SREBP site 1 protease (S1P)inhibitor with an IC of 175 nM.50Praeruptorin B is an inhibitor of sterolregulatory element-binding protei

44、ns (SREBPs).Purity: 99.32%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.95%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg HYPERLINK https:/www.MedChemE/pseudoprotodioscin.html Pseudoprotodioscin HYPERLINK https:/www.MedChemE/pseud

45、oprotodioscin.html HYPERLINK https:/www.MedChemE/C75-trans.html trans-C75Cat. No.: HY-N0686()-C75) Cat. No.: HY-12364APseudoprotodioscin, a furostanoside, inhibitsSREBP1/2 and microRNA 33a/b levels and reduces thegene expression regarding the synthesis ofcholesterol and triglycerides.trans-C75 ()-C7

46、5) is an enantiomer of C75. C75is a synthetic fatty-acid synthase (FASN)inhibitor.Purity: 98.76%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 20 mgPurity: 99.91%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERL