Any feedback?
Please rate this page
(all_enzymes.php)
(0/150)

BRENDA support

1.13.11.34: arachidonate 5-lipoxygenase

This is an abbreviated version!
For detailed information about arachidonate 5-lipoxygenase, go to the full flat file.

Word Map on EC 1.13.11.34

Reaction

(6E,8Z,11Z,14Z)-(5S)-5-hydroperoxyicosa-6,8,11,14-tetraenoate
=
leukotriene A4
+
H2O

Synonyms

5-lipoxygenase, 5-LO, 5-LO1, 5-LOX, 5DELTA-lipoxygenase, 5LO, 5LOX-1, ALOX5, arachidonate 5-LO, arachidonate:oxygen oxidoreductase, arachidonic 5-lipoxygenase, arachidonic acid 5-lipoxygenase, C-5-lipoxygenase, DELTA5-lipoxygenase, H5-LO, leukotriene A4 synthase, leukotriene-A4 synthase, lipoxygenase 15, lipoxygenase 5, lipoxygenase-1, LO-1, LOX-15, LOX-5, LTA synthase, LTA4 synthase, oxygenase, arachidonate, 5-lip-, PMNL 5-lipoxygenase

ECTree

     1 Oxidoreductases
         1.13 Acting on single donors with incorporation of molecular oxygen (oxygenases)
             1.13.11 With incorporation of two atoms of oxygen
                1.13.11.34 arachidonate 5-lipoxygenase

Inhibitors

Inhibitors on EC 1.13.11.34 - arachidonate 5-lipoxygenase

Please wait a moment until all data is loaded. This message will disappear when all data is loaded.
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(-)-epicatechin
-
-
(1-difluoromethyl-2-oxo-1,2-dihydropyridin-3-yl)acetic acid
-
-
(1-difluoromethyl-2-oxo-1,2-dihydropyridin-4-yl)acetic acid
-
-
(1-[2-[4-(trifluoromethyl)phenyl]ethyl]-1H-1,2,3-triazol-4-yl)methyl (2E)-3-(3,4-dihydroxyphenyl)prop-2-enoate
compound forms pi-pi interactions with residues Phe177, His367 and coordinates iron
-
(10E,12E)-octadeca-10,12-dien-8-ynoic acid
-
-
(11E)-octadec-11-en-9-ynoic acid
-
-
(15S)-hydroperoxy-5,8,11,13-eicosatetraenoyl lysophosphatidylcholine
-
-
(17S)-hydroperoxy-4,7,10,13,15,19-docosahexaenoyl lysophosphatidylcholine
-
-
(1E)-1-((1-[(1Z)-prop-1-en-1-yldisulfanyl]propyl)sulfinyl)prop-1-ene
-
-
(1E)-1-(2,5-dihydroxyphenyl)-5-phenylpent-1-en-3-one
inhibits leukotriene biosynthesis in isolated human neutrophils and in whole blood
-
(1E)-1-(3,4-dihydroxyphenyl)-6-phenylhex-1-en-3-one
inhibits leukotriene biosynthesis in isolated human neutrophils and in whole blood
-
(1E)-1-(4-hydroxy-3,5-dimethoxyphenyl)-5-phenylpent-1-en-3-one
inhibits leukotriene biosynthesis in isolated human neutrophils and in whole blood, retains 50% of inhibitory activity after up to one hour of incubation
-
(2,4-dihydroxyphenyl)[3-(1-[hydroxy[(3,4,5-trihydroxyphenyl)methyl]amino]ethyl)phenyl]methanone
-
(2,4-dihydroxyphenyl)[3-(1-[hydroxy[(4-hydroxyphenyl)methyl]amino]ethyl)phenyl]methanone
-
(2E)-1-(2-hydroxy-4-methoxyphenyl)-3-(2,4,5-trimethoxyphenyl)prop-2-en-1-one
-
-
(2E)-1-(2-hydroxy-4-methoxyphenyl)-3-(3,4,5-trimethoxyphenyl)prop-2-en-1-one
-
-
(2E)-1-(2-hydroxy-4-methoxyphenyl)-3-(4-hydroxyphenyl)prop-2-en-1-one
-
-
(2E)-1-(2-hydroxy-4-methoxyphenyl)-3-(4-methoxyphenyl)prop-2-en-1-one
-
-
(2E)-1-(2-hydroxy-4-methoxyphenyl)-3-[3-methoxy-4-(3-phenoxypropoxy)phenyl]prop-2-en-1-one
-
-
(2E)-1-(2-hydroxy-4-methoxyphenyl)-3-[4-(morpholin-4-ylcarbonyl)phenyl]prop-2-en-1-one
-
-
(2E)-1-(2-hydroxy-4-methoxyphenyl)-3-[4-(piperidin-1-ylcarbonyl)phenyl]prop-2-en-1-one
-
-
(2E)-1-(2-hydroxy-4-methoxyphenyl)-3-[4-(pyrrolidin-1-ylcarbonyl)phenyl]prop-2-en-1-one
-
-
(2E)-1-(2-hydroxy-4-methoxyphenyl)-3-[4-[(4-methylpiperazin-1-yl)carbonyl]phenyl]prop-2-en-1-one
-
-
(2E)-3-(3,4-dihydroxyphenyl)-1-(2,4-dimethoxyphenyl)prop-2-en-1-one
-
-
(2E)-3-(3,4-dihydroxyphenyl)prop-2-enoic acid
-
-
(2E)-3-[3-(2-ethoxyethoxy)phenyl]-1-(2-hydroxy-4-methoxyphenyl)prop-2-en-1-one
-
-
(2E)-3-[4-(2-ethoxyethoxy)phenyl]-1-(2-hydroxy-4-methoxyphenyl)prop-2-en-1-one
-
-
(2E)-3-[4-(3-ethoxypropoxy)-3-methoxyphenyl]-1-(2-hydroxy-4-methoxyphenyl)prop-2-en-1-one
-
-
(2E)-3-[4-(benzyloxy)-3-bromo-5-methoxyphenyl]-1-(2-hydroxy-4-methoxyphenyl)prop-2-en-1-one
-
-
(2E)-3-[4-(benzyloxy)phenyl]-1-(2-hydroxy-4-methoxyphenyl)prop-2-en-1-one
-
-
(2E)-3-[4-[(1E)-3-[[(2E)-3-(2,3-dihydroxyphenyl)prop-2-enoyl]oxy]prop-1-en-1-yl]phenyl]prop-2-en-1-yl (2E)-3-(3,4-dihydroxyphenyl)prop-2-enoate
caffeic acid phenylethyl ester analogue, IC50 value for inhibition of 5-Lox product synthesis in transfected HEK-293 cells is 0.00061 mM. Compound is a good radical scavenger
-
(2E,2'E)-(1,1'-(2,2-bis((4-(((E)-3-(3,4-dihydroxyphenyl)acryloyloxy)methyl)-1H-1,2,3-triazol-1-yl)methyl)propane-1,3-diyl)bis(1H-1,2,3-triazole-4,1-diyl))bis(methylene) bis(3-(3,4-dihydroxyphenyl)acrylate)
-
potent inhibition by 92%
(2E,2'E)-(1,1'-(2,2-bis((4-(cinnamoyloxymethyl)-1H-1,2,3-triazol-1-yl)methyl)propane-1,3-diyl)bis(1H-1,2,3-triazole-4,1-diyl))bis(methylene) bis(3-phenylacrylate)
-
shows less inhibitory activity than the corresponding clusters bearing the caffeic acid moiety
(2E,2'E)-(1,1'-(2-((4-(((E)-3-(3,4-dihydroxyphenyl)acryloyloxy)methyl)-1H-1,2,3-triazol-1-yl)methyl)-2-(hydroxymethyl)propane-1,3-diyl)bis(1H-1,2,3-triazole-4,1-diyl))bis(methylene) bis(3-(3,4-dihydroxyphenyl)acrylate)
-
potent inhibition by 91%
(2E,2'E)-(1,1'-(2-((4-(cinnamoyloxymethyl)-1H-1,2,3-triazol-1-yl)methyl)-2-(hydroxymethyl)propane-1,3-diyl)bis(1H-1,2,3-triazole-4,1-diyl))bis(methylene) bis(3-phenylacrylate)
-
shows less inhibitory activity than the corresponding clusters bearing the caffeic acid moiety
(2E,2'E)-2,2'-(4,4'-(2,2-bis(((1-(2-((E)-3-(3,4-dihydroxyphenyl)acryloyloxy)ethyl)-1H-1,2,3-triazol-4-yl)methoxy)methyl)propane-1,3-diyl)bis(oxy)bis(methylene)bis(1H-1,2,3-triazole-4,1-diyl))bis(ethane-2,1-diyl) bis(3-(3,4-dihydroxyphenyl)acrylate)
-
-
(2E,2'E)-2,2'-(4,4'-(2,2-bis(((1-(2-(cinnamoyloxy)ethyl)-1H-1,2,3-triazol-4-yl)methoxy)methyl)propane-1,3-diyl)bis(oxy)bis(methylene)bis(1H-1,2,3-triazole-4,1-diyl))bis(ethane-2,1-diyl) bis(3-phenylacrylate)
-
shows less inhibitory activity than the corresponding clusters bearing the caffeic acid moiety
(2E,5E)-5-[(2E)-3-(furan-2-yl)prop-2-en-1-ylidene]-3-phenyl-2-(phenylimino)-1,3-thiazolidin-4-one
-
-
(2E,6E,10E)-13-((R)-6-hydroxy-2,5,7,8-tetramethylchroman-2-yl)-N-(4-methoxybenzyl)-2,6,10-trimethyltrideca-2,6,10-trienamide
significant inhibitory activity in both cell-free and cell-based assays, inhibits leukotriene biosynthesis by human primary polymorphonuclear leukocytes, IC50 value 250 nM
-
(2E,6E,10E)-13-((R)-6-hydroxy-2,8-dimethylchroman-2-yl)-N-(4-methoxybenzyl)-2,6,10-trimethyltrideca-2,6,10-trienamide
significant inhibitory activity in both cell-free and cell-based assays, inhibits leukotriene biosynthesis by human primary polymorphonuclear leukocytes, IC50 value 184 nM
-
(2E,6E,10E)-13-(6-hydroxy-2,8-dimethylchroman-2-yl)-2,6,10-trimethyl-N-(pyridin-3-ylmethyl)trideca-2,6,10-trienamide
inhibits leukotriene biosynthesis by human primary polymorphonuclear leukocytes, IC50 value 415 nM
-
(2E,6E,10E)-N-benzyl-13-((R)-6-hydroxy-2,5,7,8-tetramethylchroman-2-yl)-2,6,10-trimethyltrideca-2,6,10-trienamide
significant inhibitory activity in both cell-free and cell-based assays, inhibits leukotriene biosynthesis by human primary polymorphonuclear leukocytes, IC50 value 173 nM
-
(2E,6E,10E)-N-benzyl-13-((R)-6-hydroxy-2,8-dimethylchroman-2-yl)-2,6,10-trimethyltrideca-2,6,10-trienamide
inhibits leukotriene biosynthesis by human primary polymorphonuclear leukocytes, IC50 value 303 nM
-
(2Z)-2-[4-(acetylamino)phenyl]-3-[4-(methylsulfonyl)phenyl]prop-2-enoic acid
-
-
(5E)-2-(3-acetylphenyl)-5-(4-methoxybenzylidene)-1,3-thiazol-4(5H)-one
-
-
(5E)-2-(3-fluorophenyl)-5-(4-methoxybenzylidene)-1,3-thiazol-4(5H)-one
-
-
(5E)-2-(4-acetylphenyl)-5-(4-methoxybenzylidene)-1,3-thiazol-4(5H)-one
-
-
(5E)-2-(4-aminophenyl)-5-(4-methoxybenzylidene)-1,3-thiazol-4(5H)-one
-
-
(5E)-2-(4-chlorophenyl)-5-(4-hydroxybenzylidene)-1,3-thiazol-4(5H)-one
-
-
(5E)-2-(4-chlorophenyl)-5-(4-methoxybenzylidene)-1,3-thiazol-4(5H)-one
-
-
(5E)-2-(4-hydroxyphenyl)-5-(4-methoxybenzylidene)-1,3-thiazol-4(5H)-one
-
-
(5E)-2-(4-methylphenyl)-5-(3,4,5-trimethoxybenzylidene)-1,3-thiazol-4(5H)-one
-
-
(5E)-5-(2,4-dimethoxybenzylidene)-2-(4-methylphenyl)-1,3-thiazol-4(5H)-one
-
-
(5E)-5-(2-hydroxy-3-methoxybenzylidene)-2-(4-methylphenyl)-1,3-thiazol-4(5H)-one
-
-
(5E)-5-(2-hydroxy-3-methoxybenzylidene)-2-phenyl-1,3-thiazol-4(5H)-one
-
-
(5E)-5-(3,5-dimethoxybenzylidene)-2-(4-methylphenyl)-1,3-thiazol-4(5H)-one
-
-
(5E)-5-(3-chloro-4-hydroxy-5-methoxybenzylidene)-2-(4-methylphenyl)-1,3-thiazol-4(5H)-one
-
-
(5E)-5-(3-chloro-4-hydroxy-5-methoxybenzylidene)-2-phenyl-1,3-thiazol-4(5H)-one
-
-
(5E)-5-(3-chloro-5-ethoxy-4-hydroxybenzylidene)-2-(4-methylphenyl)-1,3-thiazol-4(5H)-one
-
-
(5E)-5-(3-chlorobenzylidene)-2-(4-methylphenyl)-1,3-thiazol-4(5H)-one
-
-
(5E)-5-(4-hydroxy-3-methoxy-5-nitrobenzylidene)-2-phenyl-1,3-thiazol-4(5H)-one
-
-
(5E)-5-(4-methoxybenzylidene)-2-(4-methoxyphenyl)-1,3-thiazol-4(5H)-one
-
-
(5E)-5-(4-methoxybenzylidene)-2-(4-methylphenyl)-1,3-thiazol-4(5H)-one
-
-
(5E)-5-(4-methoxybenzylidene)-2-phenyl-1,3-thiazol-4(5H)-one
-
-
(5E)-5-(4-tert-butylbenzylidene)-2-phenyl-1,3-thiazol-4(5H)-one
-
-
(5E)-5-(4-[(methylperoxy)acetyl]benzylidene)-2-(4-methylphenyl)-1,3-thiazol-4(5H)-one
-
-
(5E)-5-(5-chloro-2-hydroxy-3-methoxybenzylidene)-2-phenyl-1,3-thiazol-4(5H)-one
-
-
(5E)-5-(anthracen-9-ylmethylidene)-2-phenyl-1,3-thiazol-4(5H)-one
-
-
(5E)-5-4-[(methylperoxy)acetyl]benzylidene
-
-
(5E)-5-benzylidene-2-(4-methylphenyl)-1,3-thiazol-4(5H)-one
-
-
(5E)-5-[4-(dimethylamino)benzylidene]-2-(piperidin-1-yl)-1,3-thiazol-4(5H)-one
-
-
(5S,6S,7E,9E,11Z,14Z)-5,6-epoxyicosa-7,9,11,14-tetraenoate
product inhibition
(5Z)-2-(cyclohexylamino)-5-(4-propoxybenzylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-5-(4-methoxybenzylidene)-2-(pyrrolidin-1-yl)-1,3-thiazol-4(5H)-one
-
-
(5Z)-5-(4-methylbenzylidene)-2-(naphthalen-2-ylamino)-1,3-thiazol-4(5H)-one
-
-
(5Z)-5-benzylidene-2-(phenylamino)-1,3-thiazol-4(5H)-one
-
-
(6E,8Z,11Z,14Z)-(5S)-hydroperoxyicosa-6,8,11,14-tetraenoate
-
inhibits reaction with arachidonate
(E)-N-hydroxy-N-(3-(3-phenoxyphenyl)-allyl)acetamide
-
BWA4C
(R)-N-((3-(3-fluoro-4-morpholinophenyl)-2-oxooxazolidin-5-yl) methyl)-N-hydroxyheptanamide
-
-
(R)-N-((3-(3-fluoro-4-morpholinophenyl)-2-oxooxazolidin-5-yl) methyl)-N-hydroxyoctanamide
-
-
(R)-N-((3-(3-fluoro-4-morpholinophenyl)-2-oxooxazolidin-5-yl)methyl)-N-hydroxypentanamide
-
-
(R)-N-(2-(diphenylamino)ethyl)-3-(3-(1-hydroxyureido)but-1-yn-1-yl)benzamide
dual 5-LOX/soluble epoxide hydrolase inhibitor
-
(R)-N-(3,3-bis(4-fluorophenyl)propyl)-3-(3-(1-hydroxyureido)but-1-yn-1-yl)benzamide
dual 5-LOX/soluble epoxide hydrolase inhibitor
-
([3-chloro-5-(2,3-dihydro-1H-inden-4-ylamino)phenyl]sulfanyl)acetic acid
-
-
([4-chloro-6-[(2,3-dimethylphenyl)amino]pyrimidin-2-yl]sulfanyl)(naphthalen-1-yl)acetic acid
-
-
1,10-phenanthroline
-
0.01 mM, 34% inhibition
1,4a-dimethyl-7-(propan-2-yl)-1-(prop-1-en-2-yl)-1,2,3,4,4a,4b,5,6,10,10a-decahydrophenanthrene (non-preferred name)
-
-
1-(2,4-difluorophenyl)-3-(3,5a,10-trimethyl-2-oxo-2,3,3a,4,5,5a,6,10,10a,10b-decahydrofuro[3',2':7,8]naphtho[2,3-d][1,3]thiazol-8-yl)urea
-
-
1-(2,4-dihydroxyphenyl)-2-(naphthalen-2-yl)ethanone
-
-
1-(3,4-dichlorobenzyl)-3-(2-morpholin-4-yl-2-oxoethyl)-1H-indole
82% inhibition at 0.005 mM
1-(3,4-dichlorobenzyl)-3-(3-morpholin-4-yl-3-oxopropyl)-1H-indole
38.5% inhibition at 0.005 mM
1-(3,4-difluorophenyl)-1,2,4-triazinan-3-one
-
-
1-(3-bromophenyl)-1,2,4-triazinan-3-one
-
-
1-(3-chlorophenyl)-1,2,4-triazinan-3-one
-
-
1-(3-ethylphenyl)-1,2,4-triazinan-3-one
-
-
1-(3-hydroxyphenyl)-3-[4-(methylsulfonyl)phenyl]prop-2-yn-1-one
1-(3-[5-(hydroxyureido)methyl-2-methoxyphenoxy]propyl)-3-[4-(trifluoromethoxy)phenyl]urea
KM55, a multitarget ligand and dual 5-lipoxygenase (5-LO)/soluble epoxide hydrolase (sEH) inhibitor. KM55 potently inhibits both enzymes in vitro and attenuates the formation of leukotrienes in human whole blood. It significantly inhibits the LPS-induced adhesion of leukocytes to endothelial cells by blocking leukocyte activation. Compound synthesis and evaluation, overview. KM55 inhibits the formation of leukotriene B4 and 5-hydroxyeicosatrienoic acid, while the formation of 12-hydroperoxyicosatetraenoate and 15-hydroperoxyicosatetraenoate are unaffected. KM55 blocks leukocyte-endothelial cell interaction by impairing leukocyte activation, whereas endothelial cells are not affected
1-(4-aminosulfonylphenyl)-5-(2-chloropyridin-4-yl)-3-trifluoromethyl-1H-pyrazole
-
-
1-(4-aminosulfonylphenyl)-5-[4-(1-difluoromethyl-1,2-dihydropyrid-2-one)]-3-trifluoromethyl-1H-pyrazole
-
-
1-(4-chlorobenzyl)-2-[2,2-dimethyl-3-(1H-tetrazol-5-yl)propyl]-4-methyl-6-[2-(5-phenylpyridin-2-yl)ethyl]-2,2a,4,5-tetrahydro-1H-thiopyrano[2,3,4-cd]indole
-
-
1-(4-chlorophenoxy)-3-(2-morpholin-4-yl-2-oxoethyl)-1H-indole
22% inhibition at 0.005 mM
1-(4-chlorophenoxy)-3-(3-morpholin-4-yl-3-oxopropyl)-1H-indole
26% inhibition at 0.005 mM
1-(4-chlorophenoxy)-5-methoxy-2-methyl-3-(4-morpholin-4-yl-4-oxobutyl)-1H-indole
70% inhibition at 0.005 mM
1-(4-methanesulfonylphenyl)-5-(2-chloropyridin-4-yl)-3-trifluoromethyl-1H-pyrazole
-
-
1-(4-methanesulfonylphenyl)-5-[4-(1-difluoromethyl-1,2-dihydropyrid-2-one)]-3-trifluoromethyl-1H-pyrazole
-
-
1-(4-methylbenzyl)-3-(2-morpholin-4-yl-2-oxoethyl)-1H-indole
35% inhibition at 0.005 mM
1-(4-methylbenzyl)-3-(3-morpholin-4-yl-3-oxopropyl)-1H-indole
55% inhibition at 0.005 mM
1-(6-methylpyridin-2-yl)-1,2,4-triazinan-3-one
-
-
1-(7-tert-butyl-3,3-dimethyl-2,3-dihydro-1-benzofuran-5-yl)butan-1-one
-
-
1-(8-tert-butyl-4,4-dimethyl-3,4-dihydro-2H-chromen-6-yl)-4-cyclopropylbutan-1-one
-
-
1-(benzyloxy)hept-2-yn-4-ol
-
forms three hydrogen bonds with 5-lipoxygenase
1-(difluoromethyl)-5-[[2-(methylsulfonyl)phenyl]ethynyl]pyridin-2(1H)-one
-
-
1-benzyl-3-(2-morpholin-4-yl-2-oxoethyl)-1H-indole
41% inhibition at 0.005 mM
1-benzyl-3-(3,5a,10-trimethyl-2-oxo-2,3,3a,4,5,5a,6,10,10a,10b-decahydrofuro[3',2':7,8]naphtho[2,3-d][1,3]thiazol-8-yl)urea
-
-
1-benzyl-3-(3-morpholin-4-yl-3-oxopropyl)-1H-indole
64% inhibition at 0.005 mM
1-benzyl-3-(4-morpholin-4-ylbutyl)-1H-indole
42% inhibition at 0.005 mM
1-benzyl-3-(4-oxo-4-piperazin-1-ylbutyl)-1H-indole
95% inhibition at 0.005 mM
1-benzyl-3-[2-[3-fluoro-5-(4-methoxytetrahydro-2H-pyran-4-yl)phenoxy]ethyl]-1H-indole
32% inhibition at 0.005 mM
1-benzyl-3-[3-[3-fluoro-5-(4-methoxytetrahydro-2H-pyran-4-yl)phenoxy]propyl]-5-methoxy-2-methyl-1H-indole
46.5% inhibition at 0.005 mM
1-benzyl-5-chloro-2-methyl-3-(4-morpholin-4-yl-4-oxobutyl)-1H-indole
80% inhibition at 0.005 mM
1-benzyl-5-methoxy-2-methyl-3-(4-morpholin-4-yl-4-oxobutyl)-1H-indole
54% inhibition at 0.005 mM
1-benzyl-5-methoxy-2-methyl-3-(4-oxo-4-piperazin-1-ylbutyl)-1H-indole
65% inhibition at 0.005 mM
1-hydroxy-1-[1-(5-methoxy-1-methyl-1H-indol-2-yl)ethyl]urea
-
-
1-O-dodecyl 2,3-O-isopropylidene-5,6-dideoxy-5-N-[4-(2-hydroxy-2-oxoethyl) phenylaminocarbonyl] amino-beta-L-gulofuranoside sodium salt
-
competitive inhibitor, IC50: 0.0035 mM with recombinant enzyme, IC50: 0.005 mM with native enzyme
1-phenyl-5-(propan-2-yl)-1,2,4-triazinan-3-one
-
-
1-[(4methylbenzyl)oxy]hept-2-yn-4-ol
-
is more potent than 1-(benzyloxy)hept-2-yn-4-ol to 5-lipoxygenase
1-[1-(6-tert-butyl-1-benzothiophen-2-yl)ethyl]-1-hydroxyurea
-
-
1-[3-(benzyloxy)phenyl]-1,2,4-triazinan-3-one
-
-
1-[3-(methylsulfanyl)phenyl]-3-(3,5a,10-trimethyl-2-oxo-2,3,3a,4,5,5a,6,10,10a,10b-decahydrofuro[3',2':7,8]naphtho[2,3-d][1,3]thiazol-8-yl)urea
-
-
1-[4-([3-fluoro-5-[4-(methylsulfinyl)tetrahydro-2H-pyran-4-yl]phenoxy]methyl)phenyl]-2-methyl-1H-imidazole
-
-
1-[4-([3-fluoro-5-[4-(methylsulfonyl)tetrahydro-2H-pyran-4-yl]phenoxy]methyl)phenyl]-2-methyl-1H-imidazole
-
-
10,17(S)-dihydroxydocosahexaenoic acid
-
IC50: 0.017 mM
10-nitro-oleic acid
inhibition of the 5-LO product formation of intact human polymorphonuclear leukocytes, IC50 value 0.0015 mM
-
11,14,17-Eicosatrienoic acid
11alpha,13-dihydrohelenalin acetate
-
enzyme from polymorphonuclear leukocyte
15-hydroperoxy-6,8,11,13-eicosatetraenoic acid
-
IC50: 0.0048 mM
2,3,4',5-tetrahydroxystilbene-2-O-D-glucoside
-
polymorphonuclear leukocyte
2,3-dichlorophenyl 3,5-dinitrobenzoate
-
2,5-dimethoxy-3-tridecylbenzene-1,4-diol
-
2-(1-difluoromethyl-2-oxo-1,2-dihydropyridin-3-yl)propanoic acid
-
-
2-(1-difluoromethyl-2-oxo-1,2-dihydropyridin-4-yl)phenylacetic acid
-
micromolar 5-LOX inhibitory activity
2-(1-difluoromethyl-2-oxo-1,2-dihydropyridin-4-yl)propanoic acid
-
-
2-(1-difluoromethyl-2-oxo-1,2-dihydropyridin-5-yl)acetic acid
-
-
2-(1-difluoromethyl-2-oxo-1,2-dihydropyridin-5-yl)propanoic acid
-
-
2-(2,2-dimethyl-6-(4-nitrophenyl)-7-phenyl-2,3-dihydro-1H-pyrrolizin-5-yl)acetic acid
-
-
2-(2,2-dimethyl-7-phenyl-6-(4-(trifluoromethyl)phenyl)-2,3-dihydro-1H-pyrrolizin-5-yl)acetic acid
-
-
2-(2,4-dihydroxyphenyl)-8,8-dimethyl-3-(3-methylbut-2-en-1-yl)-4H,8H-pyrano[2,3-f]chromen-4-one
-
-
2-(2-methoxyphenyl)-N-(3,5a,10-trimethyl-2-oxo-2,3,3a,4,5,5a,6,10,10a,10b-decahydrofuro[3',2':7,8]naphtho[2,3-d][1,3]thiazol-8-yl)acetamide
-
-
2-(2-[ethyl(hydroxy)amino]ethyl)dibenzo[b,e]oxepin-11(6H)-one
-
-
2-(3,4,5-trihydroxyphenyl)-3,4-dihydro-2H-chromene-3,5,7-triol
-
-
2-(3,4-dihydroxyphenyl)-3,4-dihydro-2H-chromene-3,5,7-triol
-
-
2-(3,4-dihydroxyphenyl)-3,5,7-trihydroxy-4H-chromen-4-one
-
-
2-(3-acetylphenyl)propanoic acid
-
2-(3-benzoylphenyl)propanoic acid
-
2-(3-methylbut-2-en-1-yl)-6H-[1]benzofuro[3,2-c]chromene-3,6,9-triol
-
-
2-(3-phenoxyphenyl)propanoic acid
-
2-(3-[hydroxy(methyl)amino]propyl)dibenzo[b,e]oxepin-11(6H)-one
-
-
2-(4-(biphenyl-4-ylamino)-6-chloropyrimidine-2-ylthio)octanoic acid
-
-
2-(4-(biphenyl-4-ylmethylamino)-6-chloropyrimidin-2-ylthio)octanoic acid
-
-
2-(4-chloro-6-(2,3-dimethylphenylamino)pyrimidin-2-ylthio)acetic acid
-
-
2-(4-chloro-6-(4'-cyanobiphenyl-4-ylamino)pyrimidin-2-ylthio)octanoic acid
-
-
2-(4-chloro-6-(5-methoxy-2-methylbiphenyl-4-ylamino)pyrimidin-2-ylthio)octanoic acid
-
-
2-(4-methylphenyl)-5-(2-phenylethenylidene)-1,3-thiazol-4(5H)-one
-
-
2-(5,8-dimethyl-7-propoxy-1,2,3,4-tetrahydronaphthalen-2-yl)-N-(5-methyl-1,3-thiazol-2-yl)propanamide
-
-
2-(5,8-dimethyl-7-propoxy-1,2,3,4-tetrahydronaphthalen-2-yl)-N-1,3-thiazol-2-ylpropanamide
-
-
2-(5,8-dimethyl-7-propoxy-1,2,3,4-tetrahydronaphthalen-2-yl)-N-pyridin-2-ylpropanamide
-
-
2-(5,8-dimethyl-7-propoxy-1,2,3,4-tetrahydronaphthalen-2-yl)-N-thiophen-3-ylpropanamide
-
-
2-(6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1H-pyrrolizin-5-yl)-N-(methylsulfonyl)acetamide
-
-
2-(6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1H-pyrrolizin-5-yl)-N-(phenylsulfonyl)acetamide
-
-
2-(6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1H-pyrrolizin-5-yl)-N-tosylacetamide
-
-
2-(6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1Hpyrrolizin-5-yl)-N-tosylpropanamide
-
-
2-(6-(4-chlorophenyl)-7-phenyl-2,3-dihydro-1H-pyrrolizin-5-yl)acetic acid
-
-
2-(6-(4-tert-butylphenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1H-pyrrolizin-5-yl)acetic acid
-
-
2-(7-methoxy-5,8-dimethyl-1,2,3,4-tetrahydronaphthalen-2-yl)-N-(thiophen-2-ylmethyl)propanamide
-
-
2-(7-methoxy-5,8-dimethyl-1,2,3,4-tetrahydronaphthalen-2-yl)-N-1,3-thiazol-2-ylpropanamide
-
-
2-(7-methoxy-5,8-dimethyl-1,2,3,4-tetrahydronaphthalen-2-yl)-N-pyridin-2-ylpropanamide
-
-
2-(dibenzo[b,d]furan-3-yl)-5-hydroxycyclohexa-2,5-diene-1,4-dione
-
-
2-([4-chloro-6-[(2,3-dimethylphenyl)amino]pyrimidin-2-yl]sulfanyl)octanoic acid
-
-
2-benzyl-5-hydroxycyclohexa-2,5-diene-1,4-dione
-
-
2-hexyl-5-hydroxycyclohexa-2,5-diene-1,4-dione
-
-
2-hydroxy-5-(3-nitrophenyl)cyclohexa-2,5-diene-1,4-dione
-
-
2-hydroxy-5-(naphthalen-2-ylmethyl)cyclohexa-2,5-diene-1,4-dione
-
-
2-hydroxy-5-methoxy-3-(naphthalen-2-ylmethyl)cyclohexa-2,5-diene-1,4-dione
-
-
2-methoxy-5-(naphthalen-2-yloxy)cyclohexa-2,5-diene-1,4-dione
-
-
2-methyl-3-[(morpholine-4-carbonyl)amino]-3-oxopropanoic acid
-
2-phenylethyl (2E)-3-(2,5-dihydroxyphenyl)prop-2-enoate
-
2-phenylethyl (2E)-3-(4-hydroxy-3,5-dimethoxyphenyl)prop-2-enoate
inhibits leukotriene biosynthesis in isolated human neutrophils and in whole blood
-
2-[(1-hydroxy-6-oxo-1,6-dihydropyridin-3-yl)ethynyl]benzenesulfonamide
-
-
2-[(4-[[3,5-bis(2,2,2-trifluoroethoxy)phenyl]amino]-6-chloropyrimidin-2-yl)sulfanyl]octanoic acid
-
-
2-[2-(1-difluoromethyl-2-oxo-1,2-dihydropyridin-4-yl)phenyl]propanoic acid
-
micromolar 5-LOX inhibitory activity
2-[2-[(2-methyl-1H-benzimidazol-1-yl)methyl]phenoxy]acetamide
a BRP-7 derivative
2-[2-[(2-[1-[4-(2-methylpropyl)phenyl]ethyl]-1H-benzimidazol-1-yl)methyl]phenoxy]acetamide
a BRP-7 derivative
2-[3-(1-difluoromethyl-2-oxo-1,2-dihydropyridin-4-yl)phenyl]propanoic acid
-
micromolar 5-LOX inhibitory activity
2-[3-(2-methylpropanoyl)phenyl]propanoic acid
-
2-[3-(morpholine-4-carbonyl)phenyl]propanoic acid
-
2-[3-[(4-hydroxyphenyl)carbamoyl]phenyl]propanoic acid
-
2-[3-[hydroxy(phenyl)amino]phenyl]propanoic acid
-
2-[4'-(iso-propylphenyl)-amino]-5,6-dimethyl-1,4-benzoquinone
-
potent inhibitor, IC50: 0.006 mM
2-[4'-[(morpholin-4-yl)sulfanyl][1,1'-biphenyl]-3-yl]propanoic acid
-
2-[4-(1-difluoromethyl-2-oxo-1,2-dihydropyridin-4-yl)phenyl]propanoic acid
-
micromolar 5-LOX inhibitory activity
2-[4-(morpholine-4-carbonyl)phenyl]propanoic acid
-
2-[4-([[(2E)-3-phenylprop-2-enoyl]oxy]methyl)-1H-1,2,3-triazol-1-yl]ethyl (2E)-3-(3,4-dihydroxyphenyl)prop-2-enoate
-
-
2-[5,8-dimethyl-7-(2-morpholin-4-ylethoxy)-1,2,3,4-tetrahydronaphthalen-2-yl]-N-1,3-thiazol-2-ylpropanamide
-
-
2-[6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1H-pyrrolizin-5-yl]acetic acid
-
-
2-[7-[2-(dimethylamino)ethoxy]-5,8-dimethyl-1,2,3,4-tetrahydronaphthalen-2-yl]-N-1,3-thiazol-2-ylpropanamide
-
-
2-[7-[2-(dimethylamino)ethoxy]-5,8-dimethyl-1,2,3,4-tetrahydronaphthalen-2-yl]-N-pyridin-2-ylpropanamide
-
-
2-[[5-fluoro-6-(4-fluorophenoxy)-1H-benzimidazol-2-yl]sulfanyl]-2-methylpropanoic acid
-
additionally inhibts soluble epoxide hydrolase. Compound shows potent anti-inflammatory activity and significant inhibition of edema at a dose of 100 mg/kg
-
3'-nitrobiphenyl-2,4-diol
-
-
3,4,5-trimethoxy-N-(3,5a,10-trimethyl-2-oxo-2,3,3a,4,5,5a,6,10,10a,10b-decahydrofuro[3',2':7,8]naphtho[2,3-d][1,3]thiazol-8-yl)benzamide
-
-
3,4,6-trimethoxy-5-undecylcyclohexa-2,4-dien-1-one
-
3-((naphthalene-1-yloxy)carbonyl)benzoic acid
-
3-(1,10-dihydroxydecyl)-2,5-dimethoxycyclohexa-2,5-diene-1,4-dione
-
3-(1-acetoxy-10-hydroxydecyl)-2,5-dimethoxycyclohexa-2,5-diene-1,4-dione
-
3-(1-carboxyethyl)benzoic acid
-
3-(1-difluoromethyl-2-oxo-1,2-dihydropyridin-4-yl)phenylacetic acid
-
micromolar 5-LOX inhibitory activity
3-(10-hydroxydecyl)-2,5-dimethoxycyclohexa-2,5-diene-1,4-dione
-
3-(10-hydroxydecyl)-4,5-dimethoxycyclohexa-3,5-diene-1,2-dione
-
3-(11-hydroxyundecyl)-2,5-dimethoxycyclohexa-2,5-diene-1,4-dione
-
3-(11-hydroxyundecyl)-4,5-dimethoxycyclohexa-3,5-diene-1,2-dione
-
3-(2-(2-[(4-chlorophenyl)sulfanyl]ethoxy)-3-methoxy-5-[5-(3,4,5-trimethoxyphenyl)tetrahydrofuran-2-yl]benzyl)-1-hydroxy-1-methylurea
-
-
3-(2-morpholin-4-yl-2-oxoethyl)-1-phenoxy-1H-indole
21% inhibition at 0.005 mM
3-(2-morpholin-4-yl-2-oxoethyl)-1H-indole
16% inhibition at 0.005 mM
3-(3-(1-hydroxyureido)but-1-yn-1-yl)-N-(2-(trifluoromethyl)-benzyl)benzamide
dual 5-LOX/soluble epoxide hydrolase inhibitor
-
3-(3-(1-hydroxyureido)but-1-yn-1-yl)-N-(3-phenyl-3-(4-(trifluoromethoxy)phenyl)propyl)benzamide
dual 5-LOX/soluble epoxide hydrolase inhibitor
-
3-(3-(1-hydroxyureido)but-1-yn-1-yl)-N-(4-methoxy-2-(trifluoromethyl)benzyl)-benzamide
dual 5-LOX/soluble epoxide hydrolase inhibitor
-
3-(3-(1-hydroxyureido)hex-1-yn-1-yl)-N-(2-(trifluoromethyl)-benzyl)benzamide
dual 5-LOX/soluble epoxide hydrolase inhibitor
-
3-(3-morpholin-4-yl-3-oxopropyl)-1-phenoxy-1H-indole
23% inhibition at 0.005 mM
3-(3-morpholin-4-yl-3-oxopropyl)-1H-indole
33% inhibition at 0.005 mM
3-(4,5-dihydroxy-2-methyl-9,10-dioxo-4a,9,9a,10-tetrahydroanthracen-1-yl)-2-hydroxy-4,6-dimethoxybenzoic acid
-
-
3-(4-morpholin-4-yl-4-oxobutyl)-1H-indole
62% inhibition at 0.005 mM
3-(6-(4-chlorphenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1H-pyrrolizin-5-yl)propionic acid
-
-
3-(8-hydroxyoctyl)-2,5-dimethoxycyclohexa-2,5-diene-1,4-dione
-
3-(8-hydroxyoctyl)-4,5-dimethoxycyclohexa-3,5-diene-1,2-dione
-
3-(benzyloxycarbonyl)benzoic acid
-
3-(cyclohexylmethyl)-2,5-dihydroxycyclohexa-2,5-diene-1,4-dione
-
-
3-(decahydronaphthalen-2-ylmethyl)-2,5-dihydroxycyclohexa-2,5-diene-1,4-dione
-
-
3-(naphhthalen-1-ylcarbmoyl)benzoic acid
-
3-(phenylcarbamoyl)benzoic acid
-
3-acetyl-11-keto-beta-boswellic acid
allosteric inhibitor from frankincense, wedges between the membrane-binding and catalytic domains of 5-LOX, some 30 A from the catalytic iron. Binding promotes a shift in the regiospecificity, i.e. a significant increase in the formation of 12-hydroxyeicosatetraenoic acid with the most prominent effect at 10 microM
3-benzyl-2-hydroxy-5-methoxycyclohexa-2,5-diene-1,4-dione
-
-
3-dodecyl-4,5-dimethoxybenzene-1,2-diol
-
3-dodecyl-4,5-dimethoxycyclohexa-3,5-diene-1,2-dione
-
3-ethoxy-11-oxours-12-en-23-oic acid
-
-
3-n-pentadecylcatechol
-
-
3-propylphenyl 3,5-dinitrobenzoate
-
3-tolyl 3,5-dinitrobenzoate
-
3-tridecyl-4,5-dimethoxybenzene-1,2-diol
shows anti-inflammatory effectiveness
3-undecyl-4,5-dimethoxybenzene-1,2-diol
-
3-[(10E)-pentadec-10'-en-1-yl]-catechol
-
-
3-[(10Z)-pentadec-10'-en-1-yl]-catechol
-
-
3-[2-[3-fluoro-5-(4-methoxytetrahydro-2H-pyran-4-yl)phenoxy]ethyl]-1H-indole
64% inhibition at 0.005 mM
3-[4-(3-[[(2E)-3-(2,3-dihydroxyphenyl)prop-2-enoyl]oxy]prop-1-yn-1-yl)phenyl]prop-2-yn-1-yl (2E)-3-(3,4-dihydroxyphenyl)prop-2-enoate
caffeic acid phenylethyl ester analogue, IC50 value for inhibition of 5-Lox product synthesis in transfected HEK-293 cells is 0.00036 mM. Compound is a good radical scavenger
-
3-[4-(methylsulfonyl)phenyl]-1-[4-(propan-2-yl)phenyl]prop-2-yn-1-one
-
-
3-[5-[(2E)-3,7-dimethylocta-2,6-dien-1-yl]-2,4-dihydroxyphenyl]-5,7-dihydroxy-2,3-dihydro-4H-chromen-4-one
-
-
3-[[3-fluoro-5-(4-methoxytetrahydro-2H-pyran-4-yl)phenoxy]methyl]-1-[4-(methylsulfonyl)phenyl]-5-phenyl-1H-pyrazole
-
-
4,4'-(2,3-dimethyl)-1,4-butanediylbis-1,2-benzenediol
-
-
4,5-bis(4-chlorophenyl)-1,2-selenazole
-
44% inhibition at 0.01 mM
4,5-bis(4-methoxyphenyl)-1,2-selenazole
-
58% inhibition at 0.01 mM
4,5-dimethoxy-3-tridecylcyclohexa-3,5-diene-1,2-dione
shows anti-inflammatory effectiveness
4,5-dimethoxy-3-undecylcyclohexa-3,5-diene-1,2-dione
-
4,7,10,13,16,19-docosahexaenoic acid
-
IC50: 0.0013 mM
4,9-dimethoxy-3-methyl-9,10-dihydrophenanthrene-2,7-diol
-
-
4-((3,4-dichlorobenzyl)-1H-indol-3-yl)-1-morpholinobutan-1-one
27% inhibition at 0.005 mM
4-((4-chlorobenzoyl)-1H-indol-3-yl)-1-morpholinobutan-1-one
32% inhibition at 0.005 mM
4-(1-(4-methylbenzyl)-1H-indol-3-yl)-1-morpholinobutan-1-one
34% inhibition at 0.005 mM
4-(1-benzothiophen-3-yl)benzene-1,3-diol
-
-
4-(1-benzoyl-1H-indol-3-yl)-1-morpholinobutan-1-one
58% inhibition at 0.005 mM
4-(1-benzyl-1H-indol-3-yl)-1-morpholinobutan-1-one
26% inhibition at 0.005 mM
4-(1-difluoromethyl-2-oxo-1,2-dihydropyridin-4-yl)phenylacetic acid
-
micromolar 5-LOX inhibitory activity
4-(3-(1-hydroxyureido)but-1-yn-1-yl)-N-(2-(trifluoromethyl)-benzyl)benzamide
dual 5-LOX/soluble epoxide hydrolase inhibitor, displays cellular activity in human polymorphonuclear leukocytes, oral bioavailability, and target engagement in vivo and demonstrates anti-inflammatory and anti-fibrotic efficiency in a kidney injury model caused by unilateral ureteral obstruction in mice
-
4-(3-fluoro-5-[[4-(2-methyl-1H-imidazol-1-yl)benzyl]oxy]phenyl)-N-methyltetrahydro-2H-pyran-4-carboxamide
-
-
4-(3-fluoro-5-[[4-(2-methyl-1H-imidazol-1-yl)benzyl]oxy]phenyl)tetrahydro-2H-pyran-4-ol
-
-
4-(3-fluoro-5[[4-(2-methyl-1H-imidazol-1-yl)benzyl]oxy]phenyl)tetrahydro-2H-pyran-4-carboxylic acid
-
-
4-(4-(4-chlorophenyl)thiazol-2-ylimino)cyclohexa-2,5-dienone
ST-1905
4-(4-chlorophenyl)-5-(4-methoxyphenyl)-1,2-selenazole
-
53% inhibition at 0.01 mM
4-(4-chlorophenyl)-5-p-tolyl-1,2-selenazole
-
45% inhibition at 0.01 mM
4-(4-chlorophenyl)-7-([3-fluoro-5-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]sulfanyl)-2H-chromen-2-one
-
IC50: 180 nM
4-(4-fluorophenyl)-5-(4-(methylsulfonyl)phenyl)-1,2-selenazole
-
60% inhibition at 0.01 mM
4-(4-fluorophenyl)-7-([3-fluoro-5-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenoxy]methyl)-2H-chromen-2-one
-
IC50: 55 nM
4-(4-fluorophenyl)-7-([3-fluoro-5-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]sulfanyl)-2H-chromen-2-one
-
IC50: 27 nM
4-(6-methoxynaphthalen-2-yl)butan-2-one
-
-
4-(acetyloxy)-2-[4-(acetyloxy)-6-methylhept-5-en-2-yl]cyclohexyl (2Z)-2-methylbut-2-enoate
-
-
4-(dibenzo[b,d]furan-3-yl)benzene-1,3-diol
-
-
4-(furan-3-yl)-7-[[2-(tetrahydro-2H-pyran-4-yl)pyridin-4-yl]methoxy]naphthalene-2-carbonitrile
-
-
4-(furan-3-yl)-7-[[6-(4-hydroxytetrahydro-2H-pyran-4-yl)pyridin-2-yl]methoxy]naphthalene-2-carbonitrile
-
-
4-(furan-3-yl)-7-[[7-(tetrahydro-2H-pyran-4-yl)-1,2,3,4-tetrahydroquinolin-2-yl]oxy]naphthalene-2-carbonitrile
-
-
4-(naphthalen-2-ylmethyl)benzene-1,3-diol
-
-
4-(thianthren-2-yl)benzene-1,3-diol
-
-
4-([[5-fluoro-6-(1H-1,2,4-triazol-1-yl)-1H-benzimidazol-2-yl]sulfanyl]methyl)benzoic acid
-
additionally inhibts soluble epoxide hydrolase. Compound shows potent anti-inflammatory activity and significant inhibition of edema at a dose of 100 mg/kg
-
4-([[5-fluoro-6-(4-fluorophenoxy)-1H-benzimidazol-2-yl]sulfanyl]methyl)benzoic acid
-
additionally inhibts soluble epoxide hydrolase. Compound shows potent anti-inflammatory activity and significant inhibition of edema at a dose of 100 mg/kg
-
4-([[6-(4-chlorophenoxy)-5-fluoro-1H-benzimidazol-2-yl]sulfanyl]methyl)benzoic acid
-
additionally inhibts soluble epoxide hydrolase. Compound shows potent anti-inflammatory activity and significant inhibition of edema at a dose of 100 mg/kg
-
4-benzylbenzene-1,3-diol
-
-
4-chloro-N-([4-[(2E)-3-(2,4-dichlorophenyl)prop-2-enoyl]phenyl]carbamoyl)benzenesulfonamide
-
IC50: 0.00042 mM
4-chloro-N-([4-[(2E)-3-phenylprop-2-enoyl]phenyl]carbamoyl)benzenesulfonamide
-
IC50: 0.00083 mM
4-hexylbenzene-1,3-diol
-
-
4-methoxy-4-[3-(naphthalen-2-ylmethoxy)phenyl]tetrahydro-2H-pyran
-
-
4-methoxy-N-(3,5a,10-trimethyl-2-oxo-2,3,3a,4,5,5a,6,10,10a,10b-decahydrofuro[3',2':7,8]naphtho[2,3-d][1,3]thiazol-8-yl)benzamide
-
-
4-methyl-N-(3,5a,10-trimethyl-2-oxo-2,3,3a,4,5,5a,6,10,10a,10b-decahydrofuro[3',2':7,8]naphtho[2,3-d][1,3]thiazol-8-yl)-1,2,3-thiadiazole-5-carboxamide
-
-
4-methyl-N-([4-[(2E)-3-(2,3,4-trimethylphenyl)prop-2 enoyl]phenyl]carbamoyl)benzenesulfonamide
-
IC50: 0.00045 mM
4-methyl-N-([4-[(2E)-3-phenylprop-2-enoyl]phenyl]carbamoyl)benzenesulfonamide
-
IC50: 0.00089 mM
4-methylesculetin
-
polymorphonuclear leukocyte
4-[(1E)-3-(2-hydroxy-4-methoxyphenyl)-3-oxoprop-1-en-1-yl]-N-(2-hydroxy-5-nitrophenyl)benzamide
-
-
4-[(1E)-3-(2-hydroxy-4-methoxyphenyl)-3-oxoprop-1-en-1-yl]-N-(2-hydroxyphenyl)benzamide
-
-
4-[(1E)-3-(2-hydroxy-4-methoxyphenyl)-3-oxoprop-1-en-1-yl]-N-(2-methoxyphenyl)benzamide
-
-
4-[(1E)-3-(2-hydroxy-4-methoxyphenyl)-3-oxoprop-1-en-1-yl]-N-(2-phenylethyl)benzamide
-
-
4-[(1E)-3-(2-hydroxy-4-methoxyphenyl)-3-oxoprop-1-en-1-yl]-N-(propan-2-yl)benzamide
-
-
4-[(1E)-3-(2-hydroxy-4-methoxyphenyl)-3-oxoprop-1-en-1-yl]-N-methyl-N-phenylbenzamide
-
-
4-[(1E)-3-(2-hydroxy-4-methoxyphenyl)-3-oxoprop-1-en-1-yl]-N-propylbenzamide
-
-
4-[(1E)-3-(3-phenylpropoxy)prop-1-en-1-yl]benzene-1,2-diol
caffeic acid phenylethyl ester analogue, IC50 value for inhibition of 5-Lox product synthesis in transfected HEK-293 cells is 0.00018 mM. Compound is a good radical scavenger
-
4-[(1E)-3-(benzyloxy)prop-1-en-1-yl]benzene-1,2-diol
caffeic acid phenylethyl ester analogue, IC50 value for inhibition of 5-Lox product synthesis in transfected HEK-293 cells is 0.00043 mM. Compound is a good radical scavenger
-
4-[(4-cyclohexyl-5-methyl-1,3-thiazol-2-yl)amino]-2,6-dimethylphenol
lead compound, in vitro pharmacokinetic profile, shows no cytotoxicity, overview
4-[(hydroxy[1-[3'-(morpholin-4-yl)[1,1'-biphenyl]-3-yl]ethyl]amino)methyl]phenol
-
4-[([5-fluoro-6-[4-(1H-imidazol-1-yl)phenoxy]-1H-benzimidazol-2-yl]sulfanyl)methyl]benzoic acid
-
additionally inhibts soluble epoxide hydrolase. Compound shows potent anti-inflammatory activity and significant inhibition of edema at a dose of 100 mg/kg
-
4-[1-(4-chlorobenzyl)-4-methyl-6-[(5-phenylpyridin-2-yl)methoxy]-2,2a,4,5-tetrahydro-1H-thiopyrano[2,3,4-cd]indol-2-yl]-3,3-dimethyl-N-(methylsulfonyl)butanamide
-
-
4-[4-(4-fluoro-phenyl)-thiazol-2-ylamino]-2,6-dimethylphenol
-
KR-33749, the compound exhibits a more than 1000fold selectivity for 5-LO against 12-LO and 15-LO
4-[5-(1H-indol-3-yl)-3-(trifluoromethyl)-4,5-dihydro-1H-pyrazol-1-yl]benzenesulfonamide
-
-
4-[5-(1H-indol-3-yl)-3-trifluoromethyl-4,5-dihydropyrazol-1-yl]-benzenesulfonamide
4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamide
-
-
4-[5-(6-chloro-1H-indol-3-yl)-3-trifluoromethyl-4,5-dihydropyrazol-1-yl]-benzenesulfonamide
4-[5-(7-chloro-1H-indol-3-yl)-3-trifluoromethyl-4,5-dihydropyrazol-1-yl]-benzenesulfonamide
4-[[4-(2,4-dichlorophenyl)-5-methyl-1,3-thiazol-2-yl]amino]-2,6-dimethylphenol
lead compound, in vitro pharmacokinetic profile, shows no cytotoxicity, overview
4-[[4-(4-chlorophenyl)-1,3-thiazol-2-yl]amino]phenol
-
4-[[4-(4-chlorophenyl)-1,3-thiazol-2-yl]imino]cyclohexa-2,5-dien-1-one
-
4-[[hydroxy(2-methyl-1-[3-[(morpholin-4-yl)oxy]phenyl]propyl)amino]methyl]phenol
-
5,5'-di(prop-2-en-1-yl)biphenyl-2,2'-diol
-
-
5,5-dimethyl-1-phenyl-1,2,4-triazinan-3-one
-
-
5,6-Dehydroarachidonate
-
irreversible
5,6-Methano-leukotriene A4
-
-
5,8,11,13-eicosatetraynoic acid
-
IC50: 0.028 mM
5,8,11,14,17-eicosapentaenoic acid
-
-
5-(2-[[3-(trifluoromethyl)phenyl]amino]phenyl)-1,3,4-oxadiazole-2(3H)-thione
-
-
5-(3,5-di-tert-butyl-4-hydroxybenzylidene)thiazolidin-2,4-dione
-
effective inhibitor of 5-LOX in vivo
5-(4-chlorophenyl)-4-(4-methoxyphenyl)-1,2-selenazole
-
42% inhibition at 0.01 mM
5-(4-chlorophenyl)-4-p-tolyl-1,2-selenazole
-
67% inhibition at 0.01 mM
5-(4-fluorophenyl)-1-[4-(methylsulfonyl)phenyl]-3-(trifluoromethyl)-1H-pyrazole
-
-
5-(4-methoxyphenyl)-4-p-tolyl-1,2-selenazole
-
64% inhibition at 0.01 mM
5-(7-tert-butyl-3,3-dimethyl-2,3-dihydro-1-benzofuran-5-yl)-5-oxopentanenitrile
-
-
5-amino-2-hydroxy-N-(propan-2-yl)benzamide
-
5-aminosalicylic acid derivative, additionally inhibits cyclooxygenases Cox-1 and Cox-2
-
5-amino-N-cyclohexyl-2-hydroxybenzamide
-
5-aminosalicylic acid derivative, additionally inhibits cyclooxygenases Cox-1 and Cox-2
-
5-amino-N-hexyl-2-hydroxybenzamide
-
5-aminosalicylic acid derivative, additionally inhibits cyclooxygenases Cox-1 and Cox-2
-
5-butyl-1-phenyl-1,2,4-triazinan-3-one
-
-
5-chloro-1-(4-chlorophenoxy)-2-methyl-3-(4-morpholin-4-yl-4-oxobutyl)-1H-indole
38% inhibition at 0.005 mM
5-chloro-2-methyl-3-(4-morpholin-4-yl-4-oxobutyl)-1H-indole
71% inhibition at 0.005 mM
5-ethyl-1-phenyl-1,2,4-triazinan-3-one
-
-
5-hydroperoxy-6,8,11,14-eicosatetraenoic acid
-
-
5-methoxy-2-methyl-1-(4-methylbenzyl)-3-(4-morpholin-4-yl-4-oxobutyl)-1H-indole
26% inhibition at 0.005 mM
5-methoxy-2-methyl-3-(4-morpholin-4-yl-4-oxobutyl)-1H-indole
73% inhibition at 0.005 mM
5-methoxy-3-tridecylbenzene-1,2,4-triol
-
5-[(E)-2-(4-hydroxyphenyl)ethenyl]benzene-1,3-diol
-
-
5-[[(2,5-dihydroxyphenyl)methyl]amino]-2-hydroxy-N-(4-methylphenyl)benzamide
-
5-aminosalicylic acid derivative, additionally inhibits cyclooxygenases Cox-1 and Cox-2
-
5-[[hydroxy(2-methyl-1-[3-[(morpholin-4-yl)oxy]phenyl]propyl)amino]methyl]benzene-1,2,3-triol
-
6-(trideca-1,4,7-triene-1-sulfinyl)-hex-5-enoic acid
-
-
6-ethenesulfinyl-hex-5-enoic acid
-
-
6-ethenesulfinyl-hex-5-enoic acid amide
-
-
6-hept-1-ene-1-sulfinyl-hex-5-enoic acid
-
-
6-hept-1-enylsulfanyl-hex-5-enoic acid
-
-
6-hydroxy-3,4-dimethoxy-5-undecylcyclohexa-2,4-dien-1-one
-
6-vinylsulfanyl-hex-5-enoic acid
-
-
6-vinylsulfanyl-hex-5-enoic acid amide
-
-
6-[(4-hydroxy-3,6-dioxocyclohexa-1,4-dien-1-yl)methyl]naphthalene-2-carboxylic acid
-
-
6-[[3-fluoro-5-(4-methoxytetrahydro-2H-pyran-4-yl)phenoxy]methyl]-1-methylquinolin-2(1H)-one
-
-
7,17(S)-dihydroxydocosahexaenoic acid
-
IC50: 0.007 mM
7,8-dihydroxy-2H-chromen-2-one
-
-
7-(4-methylphenyl)-6-[4-(methylsulfonyl)phenyl]-2,3-dihydro-1H-pyrrolizine
-
-
7-([3-fluoro-5-[(1R)-1-hydroxy-1-pyridin-2-ylpropyl]phenoxy]methyl)-4-furan-3-yl-2H-chromen-2-one
-
IC50: 175 nM
7-([3-fluoro-5-[(1R,3R,5S)-3-hydroxy-6,8-dioxabicyclo[3.2.1]oct-3-yl]phenoxy]methyl)-4-(4-fluorophenyl)-2H-chromen-2-one
-
-
7-([3-fluoro-5-[(1R,3R,5S)-3-hydroxy-6,8-dioxabicyclo[3.2.1]oct-3-yl]phenoxy]methyl)-4-furan-3-yl-2H-chromen-2-one
-
IC50: 200 nM
7-([3-fluoro-5-[(1R,3R,5S)-3-hydroxy-6,8-dioxabicyclo[3.2.1]oct-3-yl]phenoxy]methyl)-4-phenyl-2H-chromen-2-one
-
IC50: 300 nM
7-([3-fluoro-5-[(1S)-1-hydroxy-1-(1,3-thiazol-2-yl)propyl]phenoxy]methyl)-4-(4-fluorophenyl)-2H-chromen-2-one
-
IC50: 175 nM
7-([3-fluoro-5-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]sulfanyl)-4-furan-3-yl-2H-chromen-2-one
-
IC50: 9 nM
7-([3-fluoro-5-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]sulfanyl)-4-phenyl-2H-chromen-2-one
-
IC50: 26 nM
7-tert-butyl-N-ethyl-N,3,3-trimethyl-2,3-dihydro-1-benzofuran-5-carboxamide
-
-
7-thiaarachidonic acid
-
-
7-[[3-(1-ethyl-1-hydroxypropyl)-5-fluorophenoxy]methyl]-4-furan-3-yl-2H-chromen-2-one
-
IC50: 15 nM
7-[[3-(4-methoxytetrahydro-2H-pyran-4-yl)benzyl]oxy]-4-phenylnaphtho[2,3-c]furan-1(3H)-one
-
-
7-[[3-fluoro-5-(3-hydroxy-6,8-dioxabicyclo[3.2.1]oct-3-yl)phenoxy]methyl]-4-(furan-3-yl)quinoline-2-carbonitrile
-
-
8,11,13-cis-icosatrienoic acid
-
-
8,11,14-eicosatrienoic acid
8-hydroxyquinoline
-
0.01 mM, 59% inhibition
AA-861
AA861
ABT 761
-
CAS: 154355-76-7
ABT-761
-
-
acetonylacetone bisphenylhydrazone
-
IC50 for reaction with linoleic acid: 0.015 mM, IC50 for reaction with arachidonic acid: 0.0039 mM
arachidonate
substrate inhibition
arachidonic acid
arachidonoyl lysophosphatidylcholine
-
-
baicalein
benzaldehyde phenylhydrazone
-
IC50 for reaction with linoleic acid: 0.0345 mM, IC50 for reaction with arachidonic acid: 0.0014 mM
benzyl 2-(3-chlorobenzyl)-5-hydroxy-1H-benzo[g]indole-3-carboxylate
-
-
benzyl 2-(4-chlorobenzyl)-5-hydroxy-1H-benzo[g]indole-3-carboxylate
-
-
beta-hydroxyacteoside
-
enzyme from polymorphonuclear leukocyte
biphenyl-2,4-diol
-
-
biphenyl-3-yl 3,5-dinitrobenzoate
-
biphenyl-4-yl 3,5-dinitrobenzoate
-
BRP-7
benzimidazole derivative BRP-7 inhibits leukotriene biosynthesis in vitro and in vivo by targeting 5-lipoxygenase-activating protein (FLAP). BRP-7 blocks 5-LOX co-localization with FLAP at the nuclear envelope in neutrophils. No complete inhibition up to 0.01 mM
BW755C
BWA4C
caffeic acid
caffeic acid phenethyl ester
cannabidiol
-
-
capsaicin
-
enzyme from polymorphonuclear leukocyte
catechol
-
IC50: 0.062 mM
celecoxib
CGP28238
-
-
chalcone
inhibition of the 5-LO product formation of intact human polymorphonuclear leukocytes, IC50 value 0.006 mM
cholesterol
-
addition to a membrane preperation in vitro reduces 5-lipoxygenase activity by half. Cholesterol sulfate can inhibit 5-lipoxygenase in intact cells
Cirsiliol
CJ-13,610
-
-
CJ-13610
-
-
Cox-189
-
-
curcumin
inhibition of the 5-LO product formation of intact human polymorphonuclear leukocytes, IC50 value 0.0016 mM
cyrhetrenyl carboxylic acid
the compound is a good ROS generator
-
daidzein
-
noncompetitive
daphnetin
-
polymorphonuclear leukocyte
delphinidin 3-O-galactoside
-
from Vaccinium myrtillus berries, strong inhibitor, in a concentration-dependent manner
delphinidin 3-O-glucoside
-
from Vaccinium myrtillus berries, strong inhibitor, in a concentration-dependent manner
delta-garcinoic acid
i.e. an omega-oxidized tocotrienol, inhibits leukotriene biosynthesis by human primary polymorphonuclear leukocytes, IC50 value 345 nM
-
delta-tocopherol-13'-carboxychromanol
competitive, compound decreases leukotriene B4 from stimulated neutrophil-like cells without affecting translocation of 5-Lox from cytosol to the nucleus. Compound additionally inhibits cyclooxygenases Cox-1 and Cox-2
-
delta-tocotrienol
competitive, compound decreases leukotriene B4 from stimulated neutrophil-like cells without affecting translocation of 5-Lox from cytosol to the nucleus. Compound additionally inhibits cyclooxygenases Cox-1 and Cox-2
delta-tocotrienol-13'-carboxychromanol
competitive, compound decreases leukotriene B4 from stimulated neutrophil-like cells without affecting translocation of 5-Lox from cytosol to the nucleus. Compound additionally inhibits cyclooxygenases Cox-1 and Cox-2
-
Diamide
in 5-LO/FLAP-transfected HeLa cells, treatment with the thiol-oxidizing agent diamide which promotes glutathionylation at surface Cys residues leads to a decreased leukotriene synthesis by wild-type 5-LO
diclofenac
-
-
diphenyldisulfide
-
IC50: 0.002-0.005
docosahexaenoic acid
-
substrate inhibition
ebselen
-
54% inhibition at 0.01 mM
eicosapentaenoic acid
eltenac
-
-
embelin
epinephrine
-
IC50: 0.98 mM
ER-34122
-
-
esculetin
ethyl 1-benzyl-2-(4-chlorobenzyl)-5-hydroxy-1H-benzo[g]indole-3-carboxylate
-
-
ethyl 2-((2,4-difluorophenylthio)methyl)-5-hydroxy-1-methyl-1H-indole-3-carboxylate
-
ethyl 2-((2,6-dichlorophenylthio)methyl)-5-hydroxy-1-methyl-1H-indole-3-carboxylate
-
ethyl 2-((2,6-dimethylphenylthio)methyl)-5-hydroxy-1-methyl-1H-indole-3-carboxylate
-
ethyl 2-((3,5-dimethylphenylthio)methyl)-5-hydroxy-1-methyl-1H-indole-3-carboxylate
-
ethyl 2-((3-chlorophenylthio)methyl)-5-hydroxy-1-methyl-1H-indole-3-carboxylate
-
ethyl 2-((4-fluorophenylthio)methyl)-5-hydroxy-1-methyl-1H-indole-3-carboxylate
-
ethyl 2-(2-chlorobenzyl)-5-hydroxy-1H-benzo[g]indole-3-carboxylate
-
-
ethyl 2-(2-chlorobenzyl)-5-hydroxy-1H-indole-3-carboxylate
-
-
ethyl 2-(3-bromobenzyl)-5-hydroxy-1H-benzo[g]indole-3-carboxylate
-
-
ethyl 2-(3-chlorobenzyl)-5-hydroxy-1H-benzo[g]indole-3-carboxylate
ethyl 2-(3-chlorobenzyl)-5-hydroxy-1H-indole-3-carboxylate
-
-
ethyl 2-(3-chlorobenzyl)-5-hydroxy-1H-pyrrolo[2,3-f]quinoline-3-carboxylate
-
-
ethyl 2-(3-chlorobenzyl)-5-hydroxy-6-phenyl-1H-indole-3-carboxylate
-
-
ethyl 2-(3-chlorobenzyl)-5-methoxy-1-methyl-1H-benzo[g]-indole-3-carboxylate
-
-
ethyl 2-(3-chlorobenzyl)-5-phenyl-1H-benzo[g]indole-3-carboxylate
-
-
ethyl 2-(3-chlorobenzyl)-7,8-dimethoxy-5-hydroxy-1H-benzo[g]indole-3-carboxylate
-
-
ethyl 2-(3-chlorophenyl)-5-hydroxy-1H-benzo[g]indole-3-carboxylate
-
-
ethyl 2-(3-chlorophenyl)-5-hydroxy-1H-indole-3-carboxylate
-
-
ethyl 2-(3-fluorobenzyl)-5-hydroxy-1H-benzo[g]indole-3-carboxylate
-
-
ethyl 2-(3-methoxybenzyl)-5-hydroxy-1H-benzo[g]indole-3-carboxylate
-
-
ethyl 2-(4-bromobenzyl)-5-hydroxy-1H-benzo[g]indole-3-carboxylate
-
-
ethyl 2-(4-chlorobenzyl)-5-hydroxy-1H-benzo[g]indole-3-carboxylate
-
-
ethyl 2-(4-chlorobenzyl)-5-hydroxy-1H-indole-3-carboxylate
-
-
ethyl 2-(4-chlorophenyl)-5-hydroxy-1H-benzo[g]indole-3-carboxylate
-
-
ethyl 2-(4-chlorophenyl)-5-hydroxy-1H-indole-3-carboxylate
-
-
ethyl 2-(4-fluorobenzyl)-5-hydroxy-1H-benzo[g]indole-3-carboxylate
-
-
ethyl 2-(4-methoxybenzyl)-5-hydroxy-1H-benzo[g]indole-3-carboxylate
-
-
ethyl 2-(4-trifluoromethylbenzyl)-5-hydroxy-1H-benzo[g]indole-3-carboxylate
-
-
ethyl 2-[(3-chlorophenyl)-amino]-5-hydroxy-1H-indole-3-carboxylate
ethyl 2-[2-(3-chlorophenyl)ethyl]-5-hydroxy-1H-benzo[g]indole-3-carboxylate
-
-
ethyl 2-[2-(3-chlorophenyl)ethyl]-5-hydroxy-1H-indole-3-carboxylate
-
-
ethyl 2-[2-(4-chlorophenyl)ethyl]-5-hydroxy-1H-benzo[g]indole-3-carboxylate
-
-
ethyl 2-[2-(4-chlorophenyl)ethyl]-5-hydroxy-1H-indole-3-carboxylate
-
-
ethyl 2-[[4-chloro-6-(quinolin-6-ylamino)pyrimidin-2-yl]sulfanyl]octanoate
-
-
ethyl 5-benzoyloxy-2-(3-chlorobenzyl)-1H-benzo[g]indole-3-carboxylate
-
-
ethyl 5-hydroxy-1-methyl-2-((2-(trifluoromethyl)phenylthio)methyl)-1H-indole-3-carboxylate
-
ethyl 5-hydroxy-1-methyl-2-((4-(trifluoromethoxy)phenylthio)methyl)-1H-indole-3-carboxylate
-
ethyl 5-hydroxy-1-methyl-2-((4-(trifluoromethyl)phenylthio)methyl)-1H-indole-3-carboxylate
-
ethyl 5-hydroxy-1-methyl-2-(phenylthiomethyl)-1H-indole-3-carboxylate
-
ethyl 5-hydroxy-2-((2-methoxyphenylthio)methyl)-1-methyl-1H-indole-3-carboxylate
-
ethyl 5-hydroxy-2-((4-methoxyphenylthio)methyl)-1-methyl-1H-indole-3-carboxylate
-
ethyl 5-hydroxy-2-(mesitylthiomethyl)-1-methyl-1H-indole-3-carboxylate
-
ethyl 5-hydroxy-2-phenylethyl-1H-indole-3-carboxylate
-
-
ethyl 5-hydroxy-2-phenylpropyl-1H-benzo[g]indole-3-carboxylate
-
-
ethyl 6-biphenyl-4-yl-(3-chlorobenzyl)-5-hydroxy-1H-indole-3-carboxylate
-
-
ethyl [2-[(2-[1-[4-(2-methylpropyl)phenyl]ethyl]-1H-benzimidazol-1-yl)methyl]phenoxy]acetate
a BRP-7 derivative
etoricoxib
-
-
eugenol
-
non-competitive, reversible inhibitor, IC50: 0.026 mM
eupatilin
-
IC50: 0.098 mM
falcarindiol
-
-
ferrocenyl carboxylic acid
mixed type inhibitor. The compound shows better antioxidant activity than the antioxidant Trolox
-
forsythiaside
fraxetin
-
polymorphonuclear leukocyte
genistein
-
noncompetitive
gingerdione
-
enzyme from polymorphonuclear leukocyte
glutathione
helenalin
-
enzyme from polymorphonuclear leukocyte
hyperforin
-
-
idebenone
-
indomethacin
-
IC50: 0.36 mM
iodoacetamide
-
0.01 mM, 20% inhibition
isoriccardin C
-
-
L-651,392
-
i.e. 4-bromo-2,7-dimethoxy-3H-phenothiazin-3-one, + 1 mM NADH, IV50: 0.0003-0.0005 mM
L-651,896
-
i.e. 2,3-dihydro-6-[3-(2-hydroxymethyl)-phenyl-2-propenyl]-5-benzofuranol, IC50: 0.0003-0.0004 mM
L-656,224
L-670,630
-
IC50: 0.0004 mM
L-689,065
-
IC50: 0.0003 mM
L-697,198
-
IC50: 0.00002 mM
L-702,590
-
-
L-702,701
-
IC50: 0.0015 mM
L-739,010
-
-
L-746,530
-
IC50: 27 nM
L705,302
-
IC50: 0.00002 mM
leucocyanidol
-
polymorphonuclear leukocyte
licofelone
luteolin
inhibition of the 5-LO product formation of intact human polymorphonuclear leukocytes, IC50 value 0.0006 mM
marchantin A
-
-
marchantin B
-
-
marchantin D
-
-
marchantin E
-
-
meloxicam
-
-
methanol
-
complete inhibition at 50% v/v
methyl (4-[(5E)-5-(4-methoxybenzylidene)-4-oxo-4,5-dihydro-1,3-thiazol-2-yl]phenoxy)acetate
-
-
methyl 2-(allylamino)-1H-indole-3-carboxylate
-
-
methyl 2-(benzylamino)-1H-indole-3-carboxylate
-
-
methyl 2-(diallylamino)-1H-indole-3-carboxylate
-
-
methyl 2-[(2-chlorophenyl)amino]-1H-indole-3-carboxylate
-
-
methyl 2-[(3-bromophenyl)amino]-1H-indole-3-carboxylate
-
-
methyl 2-[(3-chlorophenyl)amino]-1H-indole-3-carboxylate
-
-
methyl 2-[(3-chlorophenyl)amino]-5-chloro-1H-indole-3-carboxylate
-
-
methyl 2-[(3-fluorophenyl)amino]-1H-indole-3-carboxylate
-
-
methyl 2-[(4-chlorophenyl)amino]-1H-indole-3-carboxylate
-
-
miogadial
-
potent inhibitor, IC50: 0.004 mM
miogatrial
-
potent inhibitor, IC50: 0.0075 mM
mithramycin
-
reduces endogenous 5-lipoxygenase in Mono Mac 6 cell, which blocks GC-boxes in the proximal part of the 5-lipoxygenase gene promoter
MK 886
-
i.e. CAS: 118414-82-7, inhibition of 5-lipoxygenase in prostate cancer cells blocks production of 5-hydroxyeicosatetraenoic acid and induces massive apoptosisin both hormone-responsive and hormone-nonresponsive prostate cancer cells
MK-886
MK886
ML-3000
-
i.e. licofelone, ML-3000 has no effect on 5-LOX product synthesis in whole-blood assay, inhibition of COX pathways does not increase the transformation of arachidonic acid by the 5-LOX pathway
myrtol
-
enzyme from RBL-1 cell
-
myxochelin A
isolated from extracts of the predatory myxobacterium Pyxidicoccus fallax HKI 727, IC50 values for inhibition of proliferative cells K-562 and HeLa are 0.3052 mM and 0.0039 mM, respectively
myxochelin C
isolated from extracts of the predatory myxobacterium Pyxidicoccus fallax HKI 727, IC50 values for inhibition of proliferative cells K-562 and HeLa are 0.424 mM and 0.0535 mM, respectively
myxochelin D
isolated from extracts of the predatory myxobacterium Pyxidicoccus fallax HKI 727, IC50 values for inhibition of proliferative cells K-562 and HeLa are above 0.5 mM
N-(2,4-dimethylphenyl)-4-[(1E)-3-(2-hydroxy-4-methoxyphenyl)-3-oxoprop-1-en-1-yl]benzamide
-
-
N-(3,4-dimethoxyphenyl)-3,5-dinitrobenzamide
-
N-(3,5a,10-trimethyl-2-oxo-2,3,3a,4,5,5a,6,10,10a,10b-decahydrofuro[3',2':7,8]naphtho[2,3-d][1,3]thiazol-8-yl)-1,3-benzodioxole-5-carboxamide
-
-
N-(3,5a,10-trimethyl-2-oxo-2,3,3a,4,5,5a,6,10,10a,10b-decahydrofuro[3',2':7,8]naphtho[2,3-d][1,3]thiazol-8-yl)cyclopentanecarboxamide
-
-
N-(3-(4-chlorophenyl)-3-phenylpropyl)-3-(3-(1-hydroxyureido)-but-1-yn-1-yl)benzamide
dual 5-LOX/soluble epoxide hydrolase inhibitor
-
N-(3-bromobenzyl)-3,5-dinitrobenzamide
-
N-(3-bromophenyl)-3,5-dinitrobenzamide
-
N-(3-chlorophenyl)-3,5-dinitrobenzamide
-
N-(3-phenoxycinnamyl)-acetohydroxamic acid
-
-
N-(4-chlorophenyl)-N-hydroxy-N'-(3-chlorophenyl)urea
-
IC50: 0.0001 mM
N-(4-methoxyphenyl)-3,5-dinitrobenzamide
-
N-(biphenyl-3-yl)-3,5-dinitrobenzamide
-
N-(furan-2-ylmethyl)-2-(7-methoxy-5,8-dimethyl-1,2,3,4-tetrahydronaphthalen-2-yl)propanamide
-
-
N-(naphthalene-1-yl)-3,5-dinitrobenzamide
-
N-([(5R)-3-[3-fluoro-4-(morpholin-4-yl)phenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl)-N-hydroxy-2-methylpropanamide
-
-
N-([(5R)-3-[3-fluoro-4-(morpholin-4-yl)phenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl)-N-hydroxycyclopropanecarboxamide
-
-
N-([4-[(2E)-3-(2,4-dichlorophenyl)prop-2-enoyl]phenyl]carbamoyl)-4-methylbenzenesulfonamide
-
IC50: 0.00045 mM
N-3-tolyl-3,5-dinitrobenzamide
-
N-benzyl-4-[(1E)-3-(2-hydroxy-4-methoxyphenyl)-3-oxoprop-1-en-1-yl]benzamide
-
-
N-butyl-5-[[(2,5-dihydroxyphenyl)methyl]amino]-2-hydroxybenzamide
-
5-aminosalicylic acid derivative, additionally inhibits cyclooxygenases Cox-1 and Cox-2
-
N-cyclohexyl-5-[(E)-[(2,5-dihydroxyphenyl)methylidene]amino]-2-hydroxybenzamide
-
5-aminosalicylic acid derivative, additionally inhibits cyclooxygenases Cox-1 and Cox-2
-
N-cyclohexyl-5-[[(2,5-dihydroxyphenyl)methyl]amino]-2-hydroxybenzamide
-
5-aminosalicylic acid derivative, additionally inhibits cyclooxygenases Cox-1 and Cox-2. Compound shows 114% anti-inflammatory activity relative to reference drug indomethacin at 4 h interval
-
N-cyclopentyl-2-[7-(2-methoxyethoxy)-5,8-dimethyl-1,2,3,4-tetrahydronaphthalen-2-yl]propanamide
-
-
N-dodecyl-4-[(1E)-3-(2-hydroxy-4-methoxyphenyl)-3-oxoprop-1-en-1-yl]benzamide
-
-
N-hexyl-5-[[(2,5-dihydroxyphenyl)methyl]amino]-2-hydroxybenzamide
-
5-aminosalicylic acid derivative, additionally inhibits cyclooxygenases Cox-1 and Cox-2
-
N-hydroxy-N-[(2E)-3-(3-phenoxyphenyl)prop-2-en-1-yl]acetamide
N-hydroxy-N-[1-(1-methyl-1H-indol-2-yl)ethyl]acetamide
-
-
N-methyl-2[4-(2,4,6-trimethylphenyl)phenyl]-propenehydroxamic acid
-
IC50: 0.0005 mM
N-phenyl-3,5-dinitrobenzamide
-
N-tert-butyl-2-(7-methoxy-5,8-dimethyl-1,2,3,4-tetrahydronaphthalen-2-yl)propanamide
-
-
N-[2-(cyclohexyloxy)-4-nitrophenyl]methanesulfonamide
-
-
N-[5-(4-fluorophenoxy)thiophen-2-yl]methanesulfonamide
-
-
naphthalen-1-yl 3,5-dinitrobenzoate
JMC-4, identified from virtual inhibitor screening
naphthalene-1-yl 3-nitrobenzoate
-
NAPQI
compound reacts with catalytically relevant cysteine residues 416 and 418
-
NEM
-
0.01 mM, 75% inhibition
nimesulide
-
-
nordihydroguaiaretic acid
nordihydroguiaraetic acid
norepinephrine
-
IC50: 0.49 mM
ochnaflavone
-
IC50: 0.0656 mM
oroxindin
-
polymorphonuclear leukocyte
paleatin B
-
-
panaxynol
-
-
parecoxib
-
-
perrottetin D
-
-
Phenidone
-
IC50: 0.005-0.01 mM
phenyl 3,5-dinitrobenzoate
-
piceid
-
polymorphonuclear leukocyte
Plumbagin
inhibition of the 5-LO product formation of intact human polymorphonuclear leukocytes, IC50 value 0.007 mM
polygodial
-
strong inhibitory activity, IC50: 0.0086 mM
primin
compound reacts with catalytically relevant cysteine residues 416 and 418, inhibition of the 5-LO product formation of intact human polymorphonuclear leukocytes, IC50 value 0.0028 mM
-
quercetagetin-7-O-beta-D-glucoside
-
polymorphonuclear leukocyte
quercetin
radulanin H
-
-
resveratrol
-
polymorphonuclear leukocyte
Rev-5901
-
competitive 5-LO inhibitor
rofecoxib
rutin
-
IC50: 0.033 mM
RWJ-63556
-
-
S-2474
-
-
SC-560
-
-
SC-756
-
-
shikonin
inhibition of the 5-LO product formation of intact human polymorphonuclear leukocytes, IC50 value 0.0015 mM
shogaol
sideritoflavone
-
polymorphonuclear leukocyte
sulindac sulfide
suspensaside
tambuletin
-
polymorphonuclear leukocyte
tepoxalin
-
-
tert-butyl 4-[4-(1-benzyl-1H-indol-3-yl)butanoyl]piperazine-1-carboxylate
38% inhibition at 0.005 mM
tert-butyl 4-[4-(1-benzyl-5-methoxy-2-methyl-1H-indol-3-yl)butanoyl]piperazine-1-carboxylate
51.5% inhibition at 0.005 mM
tert-butyl 4-[4-(1H-indol-3-yl)butanoyl]piperazine-1-carboxylate
84% inhibition at 0.005 mM
tert-butyl 4-[4-(5-methoxy-2-methyl-1H-indol-3-yl)butanoyl]piperazine-1-carboxylate
71% inhibition at 0.005 mM
thioctic acid
-
-
thymoquinone
compound reacts with catalytically relevant cysteine residues 416 and 418, inhibition of the 5-LO product formation of intact human polymorphonuclear leukocytes, IC50 value 0.0015 mM
U73122
valdecoxib
-
-
verbascoside
YS121
-
-
ZD 2138
ZD-2138
Zileutin
-
-
zileuton
ZM 230,486
-
IC50: 0.00009 mM
ZM230487
-
-
[1-(2-cyclohexylethyl)-1H-1,2,3-triazol-4-yl]methyl (2E)-3-(3,4-dihydroxyphenyl)prop-2-enoate
compound is equipotent to zileuton. It forms pi-pi interactions with residues His367, Phe421 and coordinates iron
-
[1-(2-[[(2E)-3-(3,4-dihydroxyphenyl)prop-2-enoyl]oxy]ethyl)-1H-1,2,3-triazol-4-yl]methyl (2E)-3-(3,4-dihydroxyphenyl)prop-2-enoate
-
-
[1-(2-[[(2E)-3-phenylprop-2-enoyl]oxy]ethyl)-1H-1,2,3-triazol-4-yl]methyl (2E)-3-(3,4-dihydroxyphenyl)prop-2-enoate
-
-
[1-(2-[[(2E)-3-phenylprop-2-enoyl]oxy]ethyl)-1H-1,2,3-triazol-4-yl]methyl (2E)-3-phenylprop-2-enoate
-
shows less inhibitory activity than the corresponding clusters bearing the caffeic acid moiety
[1-(3-[4-([[(2E)-3-(3,4-dihydroxyphenyl)prop-2-enoyl]oxy]methyl)-1H-1,2,3-triazol-1-yl]-2-[(3-[4-([[(2E)-3-(3,4-dihydroxyphenyl)prop-2-enoyl]oxy]methyl)-1H-1,2,3-triazol-1-yl]-2,2-bis[[4-([[(2E)-3-(3,4-dihydroxyphenyl)prop-2-enoyl]oxy]methyl)-1H-1,2,3-triazol-1-yl]methyl]propoxy)methyl]-2-[[4-([[(2E)-3-(3,4-dihydroxyphenyl)prop-2-enoyl]oxy]methyl)-1H-1,2,3-triazol-1-yl]methyl]propyl)-1H-1,2,3-triazol-4-yl]methyl (2E)-3-(3,4-dihydroxyphenyl)prop-2-enoate
-
incorporation of additional caffeoyl units in hexamer results in less potent inhibition
[1-(3-[4-([[(2E)-3-phenylprop-2-enoyl]oxy]methyl)-1H-1,2,3-triazol-1-yl]-2-[(3-[4-([[(2E)-3-phenylprop-2-enoyl]oxy]methyl)-1H-1,2,3-triazol-1-yl]-2,2-bis[[4-([[(2E)-3-phenylprop-2-enoyl]oxy]methyl)-1H-1,2,3-triazol-1-yl]methyl]propoxy)methyl]-2-[[4-([[(2E)-3-phenylprop-2-enoyl]oxy]methyl)-1H-1,2,3-triazol-1-yl]methyl]propyl)-1H-1,2,3-triazol-4-yl]methyl (2E)-3-phenylprop-2-enoate
-
shows less inhibitory activity than the corresponding clusters bearing the caffeic acid moiety
[2-[(1S,8aR)-2-formyl-5,5,8a-trimethyldecahydronaphthalen-1-yl]ethylidene]propanedial
-
-
[2-[(2-methyl-1H-benzimidazol-1-yl)methyl]phenoxy]acetyl chloride
a BRP-7 derivative
[3-(1-[hydroxy[(3,4,5-trihydroxyphenyl)methyl]amino]ethyl)phenyl](morpholin-4-yl)methanone
-
[3-(1-[hydroxy[(4-hydroxyphenyl)methyl]amino]ethyl)phenyl](morpholin-4-yl)methanone
-
[3-(bromocarbonyl)phenyl](morpholin-4-yl)acetic acid
-
additional information
-