Lipoxygenase-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/5-Lipoxygenase.html LipoxygenaseLOXLipoxygenases (LOXs) are a family of enzymes that are responsible for the metabolism of arachidonic and docosahexaenoic acidand for the formation of several eicosanoids and docosanoids, including leukotrienes, lipoxins and neu

2、roprotectins. Depending oncells redox state and other milieu conditions, these enzymes are engaged in oxidative stress and cell death mechanisms or in cellprotection. Lipoxygenases are lipid peroxidizing enzymes, implicated in the pathogenesis of inflammatory and hyperproliferativediseases, which re

3、present potential targets for pharmacological intervention.Lipoxygenases are classified on the basis of site of arachidonate oxygenation into 5-, 8-, 9-, 11-, 12- and 15-LOX. The prominentanimal LOXs are 5-LOX, 8-LOX, 12-LOX and 15-LOX, while the plant LOXs are mostly 5-LOX and 15-LOX. Among these,

4、5-LOX is themost predominant isoform associated with the formation of 5-hydroperoxyeicosatetraenoic acid (5-HpETE) and other bioactivelipid mediators.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/5-Lipoxygenase.html Lipoxygenase HYPERLINK https:/www.MedChemE/Targets/5-Lipoxygenase.html HYPERL

5、INK https:/www.MedChemE/Targets/5-Lipoxygenase.html Inhibitors, HYPERLINK https:/www.MedChemE/Targets/5-Lipoxygenase.html HYPERLINK https:/www.MedChemE/Targets/5-Lipoxygenase.html Antagonists HYPERLINK https:/www.MedChemE/Targets/5-Lipoxygenase.html HYPERLINK https:/www.MedChemE/Targets/5-Lipoxygena

6、se.html & HYPERLINK https:/www.MedChemE/Targets/5-Lipoxygenase.html HYPERLINK https:/www.MedChemE/Targets/5-Lipoxygenase.html Modulators HYPERLINK https:/www.MedChemE/11-keto-beta-boswellic-acid.html 11-Keto-beta-boswellic HYPERLINK https:/www.MedChemE/11-keto-beta-boswellic-acid.html HYPERLINK http

7、s:/www.MedChemE/11-keto-beta-boswellic-acid.html acid(11-Keto-boswellic acid) Cat. No.: HY-N2056 HYPERLINK https:/www.MedChemE/15-lox-1-inhibitor-1.html 15-LOX-1 HYPERLINK https:/www.MedChemE/15-lox-1-inhibitor-1.html HYPERLINK https:/www.MedChemE/15-lox-1-inhibitor-1.html inhibitor HYPERLINK https:

8、/www.MedChemE/15-lox-1-inhibitor-1.html HYPERLINK https:/www.MedChemE/15-lox-1-inhibitor-1.html 1Cat. No.: HY-13898911-Keto-beta-boswellic acid (11-Keto-boswellicacid) is a pentacyclic triterpenic acid of theoleogum resin from the bark of the Boswelliaserrate tree, popularly known as IndianFrankince

9、nse.15-LOX-1 inhibitor 1 is a potent inhibitor of15-LOX-1 (15-lipoxygenase-1) with an IC value50of 0.19 M. 15-LOX-1 inhibitor 1 protectsmacrophages from lipopolysaccharide-inducedcytotoxicity. 15-LOX-1 inhibitor 1 inhibits NOformation and lipid peroxidation.Purity: 99.96%Clinical Data: No Developmen

10、t ReportedSize: 5 mg, 10 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/2-5-di-tert-butylhydroquinone.html 2,5-Di-tert-butylhydroquinone HYPERLINK https:/www.MedChemE/2-5-di-tert-butylhydroquinone.html HYPERLINK https:/www.MedChemE/3-hydroxycoumarin

11、.html 3-HydroxycoumarinCat. No.: HY-W012399 Cat. No.: HY-1271702,5-Di-tert-butylhydroquinone (DTBHQ), theindirect food additive, regulates the activity of5-lipoxygenase as well as the activity of COX-2(IC =1.8 and 14.1 M for 5-LO and COX-2,50respectively) .3-hydroxycoumarin is a potent and redox inh

12、ibitorof human 15-LOX-1. 3-hydroxycoumarin is recentlydemonstrated to protect sea urchin reproductivecells against ultraviolet B damage.Purity: 99.72%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 100 mgPurity: 98.73%Clinical Data: No Development ReportedSize: 50 mg, 100 mg, 250 mg HYPERLIN

13、K https:/www.MedChemE/3-o-acetyl-11-hydroxy-beta-boswellic-acid.html 3-O-Acetyl-11-hydroxy-beta-boswellic HYPERLINK https:/www.MedChemE/3-o-acetyl-11-hydroxy-beta-boswellic-acid.html HYPERLINK https:/www.MedChemE/3-o-acetyl-11-hydroxy-beta-boswellic-acid.html acid HYPERLINK https:/www.MedChemE/3-o-a

14、cetyl-11-hydroxy-beta-boswellic-acid.html HYPERLINK https:/www.MedChemE/4_acute_,5-Dihydroxyflavone.html 4,5-DihydroxyflavoneCat. No.: HY-N7162 Cat. No.: HY-N18813-O-Acetyl-11-hydroxy-beta-boswellic acid is apotent 5-lipoxygenase (5-LO) inhibitor.4,5-Dihydroxyflavone is a soybean LOX-1 andyeast -Glu

15、cosidase inhibitor, with an K of 102.6iM for soybean LOX-1 and an IC of 66 M for50yeast -glucosidase. LOX-1 isshort for Lectin-likeoxidized low-density lipoprotein receptor-1.Purity: 98.29%Clinical Data: No Development ReportedSize: 5 mg, 10 mgPurity: 95.46%Clinical Data: No Development ReportedSize

16、: 10 mM 1 mL, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/4-mmpb.html 4-MMPB HYPERLINK https:/www.MedChemE/4-mmpb.html HYPERLINK https:/www.MedChemE/4-nitrocatechol.html 4-NitrocatecholCat. No.: HY-118480 Cat. No.: HY-W0668904-MMPB is a selective inhibitor of 15-lipoxygenase,with an IC

17、50 of 18 M. 4-MMPB has IC50s of 19.5 Mand 19.1 M for soybean 15-lipoxygenase (SLO) andhuman 15-lipoxygenase-1 (15-LOX-1), respectively.4-MMPB has potential for the research of prostatecancer.4-Nitrocatechol is a potent lipoxygenase inhibitor.Purity: 99.69%Clinical Data: No Development ReportedSize:

18、10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 g HYPERLINK https:/www.MedChemE/4-Imidazolidinone,_1-ethyl-3-4-4-_4-hydroxyphenyl_-1-piperazinylphenyl-5,5-dimethyl-2-thioxo-.html 5-Lipoxygenase-In-1 HYPERLINK https:/www.MedChemE/4-Imidazolidinone

19、,_1-ethyl-3-4-4-_4-hydroxyphenyl_-1-piperazinylphenyl-5,5-dimethyl-2-thioxo-.html HYPERLINK https:/www.MedChemE/5-o-demethylnobiletin.html 5-O-DemethylnobiletinCat. No.: HY-U00308(5-Demethylnobiletin) Cat. No.: HY-N19425-Lipoxygenase-In-1 is a 5-Lipoxygenase inhibitorextracted from patent EP 331232

20、A2, table 4,compound example 4.10.5-O-Demethylnobiletin (5-Demethylnobiletin), apolymethoxyflavone isolated from Sideritistragoriganum, is a direct inhibition of 5-LOX(IC =0.1 M), without affecting the expression of50COX-2.Purity: 98.07%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg,

21、 50 mgPurity: 99.93%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 20 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/A-69412.html A-69412 HYPERLINK https:/www.MedChemE/A-69412.html HYPERLINK https:/www.MedChemE/alox15-in-1.html ALOX15-IN-1Cat. No

22、.: HY-101945 Cat. No.: HY-143787A-69412 is a reversible, specific inhibitor of the5-lipoxygenase (5-LO). A-69412 has the potentialto treat asthma and ulcerative colitis, andpossibly other inflammatory and allergicconditions.ALOX15-IN-1 (compound 8b) is a potent inhibitor ofthe linoleate oxygenase ac

23、tivity of rabbit andhuman ALOX15 with 50s of 0.04 and 2.06 M forICALOX15 0rthologs linoleic acid (LA) andarachidonic acid (AA), respectively.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChem

24、E/alox15-in-2.html ALOX15-IN-2Cat. No.: HY-143791 HYPERLINK https:/www.MedChemE/atreleuton.html Atreleuton(ABT-761; VIA-2291) Cat. No.: HY-117853ALOX15-IN-2 (compound 8a) is a potent inhibitor ofthe linoleate oxygenase activity of rabbit andhuman ALOX15 with 50s of 1.55 and 2.79 M forICALOX15 0rthol

25、ogs linoleic acid (LA) andarachidonic acid (AA), respectively.Atreleuton (ABT-761) is a selective, reversible,and orally bioavailable 5-Lipoxygenase (5-LO)inhibitor. Atreleuton (ABT-761) exhibits potentand selective inhibition of leukotriene formation.Purity: 98%Clinical Data: No Development Reporte

26、dSize: 1 mg, 5 mgPurity: 98%Clinical Data:Size: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/AZD_4407.html AZD HYPERLINK https:/www.MedChemE/AZD_4407.html HYPERLINK https:/www.MedChemE/AZD_4407.html 4407(ZD 4407) Cat. No.: HY-U00217 HYPERLINK https:/www.MedChemE/U66858.html Bunaprolast(U66858) Cat. No.:

27、 HY-U00170AZD 4407 is a potent 5-lipoxygenase inhibitor.Bunaprolast (U66858) is a potent inhibitor ofLTB production in human whole blood.4Bunaprolast (U66858) also exhibits significantinhibition of lipoxygenase and TXB release.2Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity:

28、 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Caffeic_acid.html Caffeic HYPERLINK https:/www.MedChemE/Caffeic_acid.html HYPERLINK https:/www.MedChemE/Caffeic_acid.html acid HYPERLINK https:/www.MedChemE/Caffeic_acid.html HYPERLINK https:/www.MedChemE/cay106

29、98.html CAY10698Cat. No.: HY-N0172 Cat. No.: HY-121585Caffeic acid is an inhibitor of both TRPV1 ionchannel and 5-Lipoxygenase (5-LO).CAY10698 (compound 1) is a potent and selectiveinhibitor of 12-Lipoxygenase (12-LOX) with an IC50of 5.1 M. CAY10698 is inactive against 5-LOX,15-LOX-1, 15-LOX-2 and C

30、OX-1/2.Purity: 98.71%Clinical Data: LaunchedSize: 10 mM 1 mL, 100 mg, 5 gPurity: 98.15%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/Chebulagic-acid.html Chebulagic HYPERLINK https:/www.MedChemE/Chebulagic-acid.html HYPERLINK

31、https:/www.MedChemE/Chebulagic-acid.html acid HYPERLINK https:/www.MedChemE/Chebulagic-acid.html HYPERLINK https:/www.MedChemE/cinnamyl-3-4-dihydroxy-cyanocinnamate.html Cinnamyl-3,4-dihydroxy-cyanocinnamateCat. No.: HY-N1996(CDC) Cat. No.: HY-138688Chebulagic acid is a COX-LOX dual inhibitorisolate

32、d from the fruits of Terminalia chebulaRetz, on angiogenesis. Chebulagic acid is a M2serine to asparagine 31 mutation (S31N) inhibitorand influenza antiviral.Cinnamyl-3,4-dihydroxy-cyanocinnamate (CDC) is apotent 12/15-Lipoxygenases (LO) inhibitor.Cinnamyl-3,4-dihydroxy-cyanocinnamate has thepotenti

33、al for the research of type 1 diabetesmellitus.Purity: 99.29%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 2 mg, 5 mg, 10 mg, 25 mgPurity: 99.77%Clinical Data: No Development ReportedSize: 5 mg, 10 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/Cirsiliol.html Cirsiliol HYPERLINK https:/www

34、.MedChemE/Cirsiliol.html HYPERLINK https:/www.MedChemE/cj-13-610.html CJ-13,610Cat. No.: HY-110399 Cat. No.: HY-106200Cirsiliol is a potent and selective 5-lipoxygenaseinhibitor and a competitive low affinitybenzodiazepine receptor ligand.CJ-13,610, a nonredox-type 5-LO inhibitor, dosedependently su

35、ppresses 5-LO product formation inionophore A23187-stimulated PMNL in the absence ofexogenous AA with an IC of about 70 nM. PMNL:50polymorphonuclear leukocytes; AA: arachidonic acid.Purity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mgPurity: 98%Clinical Data: No Development ReportedSiz

36、e: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/CMI-392.html CMI-392Cat. No.: HY-19205A HYPERLINK https:/www.MedChemE/CMI977.html CMI977(LDP977) Cat. No.: HY-U00260CMI-392 is a dual 5-lipoxygenese inhibitor andplatelet-activating factor (PAF) receptorantagonist with IC s of 100 and 10 nM,50respectively.

37、CMI977 is a potent 5-Lipoxygenase (5-LO)inhibitor.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Urea,_N-3-5-_4-fluorophenyl_methyl-2-thienyl-1-methyl-2-propyn-1-yl-N-hydroxy-.html COX/5

38、-LO-IN-1(Atreleuton analog) Cat. No.: HY-U00347 HYPERLINK https:/www.MedChemE/Docebenone.html Docebenone(AA 861) Cat. No.: HY-12886COX/5-LO-IN-1 (Atreleuton analog) is an inhibitorof cylooxygenase and 5-lipoxygenase (5-LO), usedfor the research of inflammatory and allergicdisease states.Docebenone (

39、AA 861) is a potent, selective andorally active 5-LO (5-lipoxygenase) inhibitor.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.10%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/Enazadrem.html Enazadrem HYP

40、ERLINK https:/www.MedChemE/Enazadrem.html HYPERLINK https:/www.MedChemE/fpl-62064.html FPL HYPERLINK https:/www.MedChemE/fpl-62064.html HYPERLINK https:/www.MedChemE/fpl-62064.html 62064Cat. No.: HY-U00024 Cat. No.: HY-105024Enazadrem is a 5-lipoxygenase inhibitor withantiinflammatory activities.FPL

41、 62064 is a potent 5-lipoxygenase (5-LOX) andCOX dual inhibitor, with IC values of 3.5 M50and 3.1 M for RBL-1 cytosolic 5-lipoxygenase andprostaglandin synthetase (cyclooxygenase),respectively. FPL 62064 has potentanti-inflammatory activity.Purity: 97.26%Clinical Data: No Development ReportedSize: 1

42、 mg, 5 mgPurity: 98.46%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/hz52.html HZ52 HYPERLINK https:/www.MedChemE/hz52.html HYPERLINK https:/www.MedChemE/ICI_211965.html ICI HYPERLINK https:/www.MedChemE/ICI_211965.html HYPERLINK https:/www.

43、MedChemE/ICI_211965.html 211965Cat. No.: HY-112553(ZM-211965) Cat. No.: HY-100148HZ52 is a potent, reversible 5-lipoxygenaseinhibitor, blocking leukotriene synthesis with anIC of 0.7 M in intact human polymorphonuclear50leukocytes.ICI 211965 (ZM-211965) is a selective and orallypotent 5-Lipoxygenase

44、 (5-LPO) inhibitor.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/Indirubin-3_acute_-monoxime.html Indirubin-3-monoxime(Indirubi

45、n-3-oxime) Cat. No.: HY-19807 HYPERLINK https:/www.MedChemE/isothymusin.html IsothymusinCat. No.: HY-N3451Indirubin-3-monoxime is a potent GSK-3inhibitor, and weakly inhibits 5-Lipoxygenase, withIC s of 22 nM and 7.8-10 M, respectively;50Indirubin-3-monoxime also shows inhibitoryactivities against C

46、DK5/p25 and CDK1/cyclin B,with IC s of 100 and 180 nM.50Purity: 99.89%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mgIsothymusin is a potent anti-oxidant agent.Isothymusin shows radical scavenging activities.Isothymusin shows anti-proliferative activities incancer cell lin

47、es.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/licofelone.html Licofelone(ML-3000) Cat. No.: HY-B1452 HYPERLINK https:/www.MedChemE/licofelone-d4.html Licofelone-d4Cat. No.: HY-B1452SLicofelone (ML-3000) is a dual COX/5-lipoxygenase(5-LOX) inhibito

48、r (IC =0.21/0.18 M,50respectively) for the treatment of osteoarthritis.Licofelone exerts anti-inflammatory andanti-proliferative effects.Licofelone-d4 (ML-3000-d4) is the deuteriumlabeled Licofelone. Licofelone (ML-3000) is a dualCOX/5-lipoxygenase (5-LOX) inhibitor(IC =0.21/0.18 M, respectively) fo

49、r the50treatment of osteoarthritis.Purity: 98.04%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mgPurity: 98%Clinical Data:Size: 5 mg HYPERLINK https:/www.MedChemE/RS4317.html Lonapalene(RS4317) Cat. No.: HY-U00156 HYPERLINK https:/www.MedChemE/LP117.html LP117Cat. No.: HY-U0

50、0438Lonapalene (RS4317) is a topically effective5-lipoxygenase (5-LO) inhibitor.LP117 is a novel and potent inhibitor of5-Lipoxygenase (5-LO) product synthesis with anIC of 1.1 M.50Purity: 99.07%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mgPurity: 98%Clinical Data: No Dev

51、elopment ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/LY_178002.html LY HYPERLINK https:/www.MedChemE/LY_178002.html HYPERLINK https:/www.MedChemE/LY_178002.html 178002 HYPERLINK https:/www.MedChemE/LY_178002.html HYPERLINK https:/www.MedChemE/lycopodine.html LycopodineCat. No.: HY-101579

52、Cat. No.: HY-114372LY 178002 is a potent inhibitor of 5-lipoxygenase(5-LPO), phospholipase A2, with IC of 0.6 M50for 5-lipoxygenase, inhibits cellular productionof LTB4 by human polymorphonuclear leukocytes, andshows relatively weak inhibition on cyclooxygenase.Lycopodine, a pharmacologically import

53、antbioactive component derived from Lycopodiumclavatumspores, triggers apoptosis by modulating5-lipoxygenase, and depolarizing mitochondrialmembrane potential in refractory prostate cancercells without modulating p53 activity.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 9

54、8%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/malotilate.html Malotilate HYPERLINK https:/www.MedChemE/malotilate.html HYPERLINK https:/www.MedChemE/ml351.html ML351(NKK 105) Cat. No.: HY-A0060Cat. No.: HY-111310Malotilate (NKK 105), an orally activehepatotro

55、pic agent and an anti-fibrotic substance,selectively inhibits the 5-lipoxygenase (5-LOX)(IC =4.7 M).50ML351 is a potent and highly specific 15-LOX-1inhibitor with an IC of 200 nM. ML351 shows50excellent selectivity (250-fold) versus therelated isozymes, 5-LOX, platelet 12-LOX,15-LOX-2, ovine COX-1,

56、and human COX-2.Purity: 99.54%Clinical Data: LaunchedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mgPurity: 98.19%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgwww.MedChemE 5 HYPERLINK https:/www.MedChemE/ML355.html ML355Cat. No.: HY-12341 HYPERLINK https:/www.MedChemE/nordihyd

57、roguaiaretic-acid.html Nordihydroguaiaretic HYPERLINK https:/www.MedChemE/nordihydroguaiaretic-acid.html HYPERLINK https:/www.MedChemE/nordihydroguaiaretic-acid.html acid(NDGA) Cat. No.: HY-N0198ML355 is a potent and selective inhibitor of12-Lipoxygenase (12-LOX) with an IC of 0.34 M,50shows excelle

58、nt selectivity over relatedlipoxygenases and cyclooxygenases, and possessesfavorable ADME properties.Nordihydroguaiaretic acid is a 5-lipoxygenase(5LOX) (IC =8 M) and tyrosine kinase inhibitor.50Purity: 98.42%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 9

59、9.88%Clinical Data: Phase 2Size: 10 mM 1 mL, 100 mg, 250 mg HYPERLINK https:/www.MedChemE/pectolinarigenin.html PectolinarigeninCat. No.: HY-N0493 HYPERLINK https:/www.MedChemE/pf-4191834.html PF-4191834(PF-04191834) Cat. No.: HY-117048Pectolinarigenin is a dual inhibitor ofCOX-2/5-LOX. Anti-inflamm

60、atory activity.Pectolinarigenin has potent inhibitory activitieson melanogenesis.PF-4191834 (PF-04191834) is an orally active,noniron chelating, and non-redox inhibitor of the5-Lipoxygenase (5-LOX) (IC =229 nM), displays50300-fold selectivity for 5-LOX over 12-LOX and15-LOX, shows no activity toward