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(+)-catechin hydrate
-
inhibition of isozymes GST M1-1 and M2-2
(+)-limonene oxide
about 85% inhibition at 0.1 mM
(-)-limonene oxide
about 15% inhibition at 0.1 mM
(17-chloro-3b-hydroxy-androsta-5,16-diene)-succinyl-glutathione
-
-
(2R,3S)-2-(3,4-dihydroxyphenyl)-3,4-dihydro-2H-chromene-3,5,7-triol
-
a coumaroflavan from Treculia africana, 26% total inhibition at 0.033 mM
(2Z)-2-[(4-methoxyphenyl)carbonyl]-3-(2,3,4-trimethoxyphenyl)prop-2-enoic acid
-
-
(2Z)-2-[(4-methylphenyl)carbonyl]-3-(2,3,4-trimethoxyphenyl)prop-2-enoic acid
-
-
(2Z)-2-[(4-methylphenyl)carbonyl]-3-phenylprop-2-enoic acid
-
8.1% inhibition at 0.02 mM
(2Z)-3-(1,3-benzodioxol-5-yl)-2-[(4-methoxyphenyl)carbonyl]prop-2-enoic acid
-
10% inhibition at 0.02 mM
(2Z)-3-(1,3-benzodioxol-5-yl)-2-[(4-methylphenyl)carbonyl]prop-2-enoic acid
-
9.6% inhibition at 0.02 mM
(2Z)-3-(2-methylphenyl)-2-[(4-methylphenyl)carbonyl]prop-2-enoic acid
-
9.3% inhibition at 0.02 mM
(2Z)-3-(3,4-dihydroxyphenyl)-2-[(4-methoxyphenyl)carbonyl]prop-2-enoic acid
-
-
(2Z)-3-(3,4-dihydroxyphenyl)-2-[(4-methylphenyl)carbonyl]prop-2-enoic acid
-
-
(2Z)-3-(3-hydroxyphenyl)-2-[(4-methoxyphenyl)carbonyl]prop-2-enoic acid
-
6.6% inhibition at 0.02 mM
(2Z)-3-(3-hydroxyphenyl)-2-[(4-methylphenyl)carbonyl]prop-2-enoic acid
-
13.9% inhibition at 0.02 mM
(2Z)-3-(3-methoxyphenyl)-2-[(4-methylphenyl)carbonyl]prop-2-enoic acid
-
19.0% inhibition at 0.02 mM
(2Z)-3-(4-chlorophenyl)-2-[(4-methoxyphenyl)carbonyl]prop-2-enoic acid
-
14.4% inhibition at 0.02 mM
(2Z)-3-(4-chlorophenyl)-2-[(4-methylphenyl)carbonyl]prop-2-enoic acid
-
14.4% inhibition at 0.02 mM
(2Z)-3-(4-fluorophenyl)-2-[(4-methylphenyl)carbonyl]prop-2-enoic acid
-
-
(2Z)-3-(4-hydroxy-3-methoxyphenyl)-2-[(4-methylphenyl)carbonyl]prop-2-enoic acid
-
8.8% inhibition at 0.02 mM
(2Z)-3-(4-hydroxyphenyl)-2-[(4-methylphenyl)carbonyl]prop-2-enoic acid
-
12.5% inhibition at 0.02 mM
(2Z)-3-(4-methoxyphenyl)-2-[(4-methylphenyl)carbonyl]prop-2-enoic acid
-
-
(2Z)-3-(4-methylphenyl)-2-[(4-methylphenyl)carbonyl]prop-2-enoic acid
-
-
(2Z)-3-[4-(dimethylamino)phenyl]-2-[(4-methylphenyl)carbonyl]prop-2-enoic acid
-
9.3% inhibition at 0.02 mM
(4-chloro-3-(N,N-dimethylsulfamoyl)phenyl)methanesulfonyl fluoride
-
-
(4S,6Z,10Z,11aS)-4-ethoxy-6-(hydroxymethyl)-3-methylidene-10-propoxy-3a,4,5,8,9,11a-hexahydrocyclodeca[b]furan-2(3H)-one
-
a sesquiterpene lactone from Dicoma anomala collected from Namibia, 75% total inhibition at 0.033 mM
(E)-2-(4-chloro-3-(N,N-dimethylsulfamoyl)phenyl)ethene-1-sulfonyl fluoride
-
-
(E)-N-(4-chloro-3-(N,N-dimethylsulfamoyl)phenyl)but-2-enamide
-
-
(R)-carvone
about 8% inhibition at 0.1 mM
(S)-2-amino-4-cyanobutyric acid
-
-
1,2-dichloro-4-nitrobenzene
-
1 mM, 53.3% inhibition of wild-type enzyme, 40.4% of mutant enzyme H144A, 42.4% of mutant enzyme V147A, 54.3% of mutant enzyme V147L, 35.9% of mutant enzyme R96A
1,3-Bis-(2-chloroethyl)-1-nitrosourea
-
competitive
1,7-dihydroxyanthracen-9(10H)-one
-
a xanthone from Mammea africana, 21% total inhibition at 0.033 mM
1-(4-benzylpiperidin-1-yl)prop-2-en-1-one
-
1-(4-phenylpiperidin-1-yl)prop-2-en-1-one
-
1-Amino-4-{[4-({4-chloro-6-[(2-sulfophenyl)amino]-1,3,5-triazin-2-yl}amino)-3-sulfophenyl]amino}-9,10-dioxo-9,10-dihydro-2-anthracenesulfonic acid
1-chloro-2,3-dinitrobenzene
-
-
1-chloro-2,4-dinitrobenzene
1-methyl-2-[((2-nitrobenzyl)sulfonyl)]-1H-pyrrole
-
44.3% inhibition at 0.1 mM
1-methyl-2-[(2-nitrobenzyl)sulfanyl]-1H-pyrrole
-
-
11(13)germacratrien-12,6-olide
55% inhibition at 0.033 mM
2,3,4,5-tetrahydroxy-6H-benzo[7]annulen-6-one
-
50% inhibition at 0.0052 mM
2,3,5,6-tetrachloro-1,4-benzoquinone
-
i.e. TCBQ, inhibition of GSTA1-2 and GSTA1-1 by 70-80%, and GSTA2-2 by 25%, binds to cysteine residues of the enzyme, e.g. Cys17 of GSTA1-1, via a first reversible step to covalent binding, overview, Kitz-Wilson inactivation model
2,4,6-trichloroanisole
about 5% inhibition at 0.1 mM
2,4,6-Trinitrobenzenesulfonate
-
-
2,5-dibenzylidenecyclopentanone
2,6-dibenzylidenecyclohexanone
2-(3,4-dihydroxyphenyl)-3,4-dihydro-2H-chromene-3,7-diol
85% inhibition at 0.1 mM
2-(4-chloro-3-(N,N-dimethylsulfamoyl)phenyl)ethane-1-sulfonyl fluoride
-
-
2-(4-chlorophenyl)-6-[(fluorosulfonyl)oxy]quinoline-4-carboxylic acid
-
2-(7-nitro-2,1,3-benzoxadiazol-4-ylthio)imidazole
-
-
2-([(1-methyl-1H-pyrrol-2-yl)sulfonyl]methyl)-N-((1E)-[4-(trifluoromethyl)phenyl]methylene)aniline
-
68.4% inhibition at 0.1 mM
2-([(1-methyl-1H-pyrrol-2-yl)sulfonyl]methyl)-N-[(1E)-(4-nitrophenyl)methylene]aniline
-
90.0% inhibition at 0.1 mM
2-([(1-methyl-1H-pyrrol-2-yl)sulfonyl]methyl)-N-[(1E)-(phenyl)methylene]aniline
-
30.2% inhibition at 0.1 mM
2-([(1-methyl-1H-pyrrol-2-yl)sulfonyl]methyl)-N-[(1E)-1H-pyrrol-2-ylmethylene]aniline
-
36.0% inhibition at 0.1 mM
2-butanethiol
about 2% inhibition at 0.01 mM
2-chloro-5-((cyanomethyl)amino)-N,N-dimethylbenzenesulfonamide
-
-
2-chloro-N,N-dimethyl-5 -(oxiran-2-ylmethyl) -benzenesulfonamide
-
-
2-chloro-N,N-dimethyl-5-(oxiran-2-yl)benzenesulfonamide
-
-
2-chloro-N,N-dimethyl-5-(vinylsulfonamido)-benzenesulfonamide
-
2-chloro-N-(2-(N,N-dimethylsulfamoyl)-[1,1'-biphenyl]-4-yl)-acetamide
-
-
2-chloro-N-(3-(morpholinosulfonyl)-4-(trifluoromethyl)phenyl)-acetamide
-
-
2-chloro-N-(3-(N,N-dimethylsulfamoyl)-4-(trifluoromethoxy)-phenyl)acetamide
-
-
2-chloro-N-(3-(N,N-dimethylsulfamoyl)-4-(trifluoromethyl)-phenyl)acetamide
-
-
2-chloro-N-(3-(N,N-dimethylsulfamoyl)-4-iodophenyl)-acetamide
-
-
2-chloro-N-(4-(2-hydroxyphenyl)thiazol-2-yl)-N-((3-methylisoxazol-5-yl)methyl)acetamide
-
2-chloro-N-(4-chloro-3-(morpholinosulfonyl)phenyl)acetamide
-
-
2-chloro-N-(4-chloro-3-(N,N-dimethylsulfamoyl)phenyl)-propanamide
-
-
2-chloro-N-(4-chloro-3-(N-((tetrahydrofuran-2-yl)methyl)-sulfamoyl)phenyl)acetamide
-
-
2-chloro-N-(4-chloro-3-(N-(2-hydroxyethyl)-N-methylsulfamoyl)phenyl)acetamide
-
-
2-chloro-N-(4-chloro-3-(N-(2-hydroxyethyl)sulfamoyl)phenyl)-acetamide
-
-
2-chloro-N-(4-chloro-3-(N-(2-methoxyethyl)-N-methylsulfamoyl)phenyl)acetamide
-
-
2-chloro-N-(4-chloro-3-(N-(2-methoxyethyl)sulfamoyl)phenyl)-acetamide
-
-
2-chloro-N-(4-chloro-3-(N-(3-methoxypropyl)-N-methylsulfamoyl)phenyl)acetamide
-
-
2-chloro-N-(4-chloro-3-(N-(3-methoxypropyl)sulfamoyl)phenyl)-acetamide
-
-
2-chloro-N-(4-chloro-3-(N-(tetrahydrofuran-3-yl)sulfamoyl)-phenyl)acetamide
-
-
2-chloro-N-(4-chloro-3-(N-isopropylsulfamoyl)phenyl)-acetamide
-
-
2-chloro-N-(4-chloro-3-(N-methylsulfamoyl)phenyl)acetamide
-
-
2-chloro-N-methyl-N-[(1-phenyl-1H-pyrazol-3-yl)methyl]acetamide
i.e. C4-10
2-chloro-N-[2-(cyclohexylamino)-2-oxo-1-(pyridin-2-yl)ethyl]-N-(3-fluorophenyl)acetamide
i.e. KT53
2-chloro-N-[4-chloro-3-(N,N-dimethylsulfamoyl)phenyl]acetamide
2-fluoro-N-[(1,2,3,5,6,7-hexahydro-s-indacen-4-yl)carbamoyl]-5-(oxiran-2-yl)benzene-1-sulfonamide
i.e. CRID2
2-hydroxyanthracen-9(10H)-one
-
a xanthone Mammea from africana, 38% total inhibition at 0.033 mM
2-mercaptoethanol
-
50% inhibition at 4 mM
2-methyl-1,4-naphthoquinone
3.9% to 43.2% inhibition at 0.025 mM to 0.2 mM
2-[(1-methyl-1H-pyrrol-2-ylsulfonyl)methyl]aniline
-
28.0% inhibition at 0.1 mM
2-[4-[(2E)-3-(2-bromophenyl)prop-2-enoyl]phenyl]-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione
Coturnix sp.
-
noncompetitive inhibition
2-[4-[(2E)-3-(2-chlorophenyl)prop-2-enoyl]phenyl]-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione
Coturnix sp.
-
noncompetitive inhibition
2-[4-[(2E)-3-(3-bromophenyl)prop-2-enoyl]phenyl]-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione
Coturnix sp.
-
-
2-[4-[(2E)-3-(3-chlorophenyl)prop-2-enoyl]phenyl]-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione
Coturnix sp.
-
-
2-[4-[(2E)-3-(4-bromophenyl)prop-2-enoyl]phenyl]-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione
Coturnix sp.
-
competitive inhibition
2-[4-[(2E)-3-(4-chlorophenyl)prop-2-enoyl]phenyl]-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione
Coturnix sp.
-
noncompetitive inhibition
2-[4-[(2E)-3-(4-methylphenyl)prop-2-enoyl]phenyl]-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione
Coturnix sp.
-
noncompetitive inhibition
3,3',5,5'-tetrabromophenolphthalein
-
-
3-(3,4-dihydroxybenzoyl)-4-hydroxy-8-methyl-1,5,7-tris(3-methylbut-2-en-1-yl)-8-(4-methylpent-3-en-1-yl)bicyclo[3.3.1]non-3-ene-2,9-dione
-
a benzophenone Garcinia smeathmannii, 41% total inhibition at 0.033 mM
3-(3,4-dihydroxybenzoyl)-4-hydroxy-8-methyl-5,7-bis(3-methylbut-2-enyl)-8-(4-methylpent-3-enyl)bicyclo[3.3.1]nonane-2,9-dione
95% inhibition at 0.033 mM
3-(4-chloro-3-(N,N-dimethylsulfamoyl)phenyl)propane-1-sulfonyl fluoride
-
-
3-(7-nitro-2,1,3-benzoxadiazol-4-ylthio)propionic acid
-
-
3-chloro-N-(4-chloro-3-(N,N-dimethylsulfamoyl)phenyl)-propenamide
-
-
3-ethyl-2-oxo-3,3a,7a,9b-tetrahydro-2H,4aH-1,4,5-trioxadicyclopenta[a,hi]indene-7-carboxylic acid
-
an iridoid from Plumeeria rubra, 51% total inhibition at 0.033 mM
4,4'-dichlorodiphenyltrichloroethane
-
-
4-(7-nitro-2,1,3-benzoxadiazol-4-ylthio)butanol
-
-
4-(acryloylamino)-N-(5-[[5-([5-[(2-carbamimidamidoethyl)carbamoyl]-1-methyl-1H-pyrrol-3-yl]carbamoyl)-1-methyl-1H-pyrrol-3-yl]carbamoyl]-1-methyl-1H-pyrrol-3-yl)-1-methyl-1H-pyrrole-2-carboxamide
-
a brostallicin derivative, the debrominated derivative of brostallicin is almost completely ineffective as an inhibitor of GSTP1-1
4-nitrophenethyl bromide
-
0.1 mM, 40.1% inhibition of wild-type enzyme, 23.6% of mutant enzyme H144A, 19.5% of mutant enzyme V147A, 31.4% of mutant enzyme V147L, 27.3% of mutant enzyme R96A
4-[(2-bromoacryloyl)amino]-N-(5-[[5-([5-[(2-carbamimidamidoethyl)carbamoyl]-1-methyl-1H-pyrrol-3-yl]carbamoyl)-1-methyl-1H-pyrrol-3-yl]carbamoyl]-1-methyl-1H-pyrrol-3-yl)-1-methyl-1H-pyrrole-2-carboxamide
-
i.e. brostallicin, mixed-type inhibition, inhibits GSTP1-1 and GSTM2-2, thereby being much more efficient in inhibiting GSTM2-2 than in inhibiting GSTP1-1. Brostallicin sensitivity for brostallicin is higher in cells overexpressing either the GST-pi or the GST-mu gene
4-[3-(5,5-dimethyl-4-oxo-4,5-dihydrofuran-2-yl)-3-hydroxybutoxy]-7H-furo[3,2-g]chromen-7-one
5,7-dihydroxy-6-(2-hydroxybutanoyl)-8-(3-methylbut-2-en-1-yl)-4-propyl-2H-chromen-2-one
-
a coumarin from Mammea africana, 33% total inhibition at 0.033 mM
5,8-dihydroxy-1-(hydroxymethyl)naphtho[2,3-c]furan-4,9-dione
5,8-dihydroxy-1-methylnaphtho[2,3-c]furan-4,9-dione
85% inhibition at 0.1 mM
5-(chloromethyl)-3-oxo-3H-spiro[[2]benzofuran-1,9'-xanthene]-3',6'-diyl diacetate
i.e. CMFDA
5-[2,3-dichloro-4-(2-methylene-1-oxobutyl)phenoxymethyl]-3-(4-chlorobenzyl)-1,2,4-oxadiazol
-
-
5-[2,3-dichloro-4-(2-methylene-1-oxobutyl)phenoxymethyl]-3-(4-fluorophenyl)-1,2,4-oxadiazol
-
-
5-[2,3-dichloro-4-(2-methylene-1-oxobutyl)phenoxymethyl]-3-(4-methoxyphenyl)-1,2,4-oxadiazol
-
-
5-[2,3-dichloro-4-(2-methylene-1-oxobutyl)phenoxymethyl]-3-(4-nitrobenzyl)-1,2,4-oxadiazol
-
-
5-[2,3-dichloro-4-(2-methylene-1-oxobutyl)phenoxymethyl]-3-(4-trifluoromethylphenyl)-1,2,4-oxadiazol
-
-
5-[2,3-dichloro-4-(2-methylene-1-oxobutyl)phenoxymethyl]-3-methyl-1,2,4-oxadiazol
-
-
5-[2,3-dichloro-4-(2-methylene-1-oxobutyl)phenoxymethyl]-3-phenyl-1,2,4-oxadiazol
-
-
5-[2,3-dimethyl-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-(4-chlorobenzyl)-1,2,4-oxadiazol
-
-
5-[2,3-dimethyl-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-(4-fluorophenyl)-1,2,4-oxadiazol
-
-
5-[2,3-dimethyl-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-(4-hydroxyphenyl)-1,2,4-oxadiazol
-
-
5-[2,3-dimethyl-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-(4-nitrobenzyl)-1,2,4-oxadiazol
-
-
5-[2,3-dimethyl-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-(4-trifluoromethylphenyl)-1,2,4-oxadiazol
-
-
5-[2,3-dimethyl-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-methyl-1,2,4-oxadiazol
-
-
5-[2,3-dimethyl-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-phenyl-1,2,4-oxadiazol
-
-
5-[3-bromo-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-(4-fluorophenyl)-1,2,4-oxadiazol
-
-
5-[3-bromo-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-(4-trifluoromethylphenyl)-1,2,4-oxadiazol
-
-
5-[3-bromo-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-methyl-1,2,4-oxadiazol
-
-
5-[3-bromo-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-phenyl-1,2,4-oxadiazol
-
-
5-[3-chloro-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-(4-fluorophenyl)-1,2,4-oxadiazol
-
-
5-[3-chloro-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-(4-trifluoromethylphenyl)-1,2,4-oxadiazol
-
-
5-[3-chloro-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-methyl-1,2,4-oxadiazol
-
-
5-[3-chloro-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-phenyl-1,2,4-oxadiazol
-
-
5-[3-methyl-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-(4-fluorophenyl)-1,2,4-oxadiazol
-
-
5-[3-methyl-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-(4-hydroxyphenyl)-1,2,4-oxadiazol
-
-
5-[3-methyl-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-(4-nitrobenzyl)-1,2,4-oxadiazol
-
-
5-[3-methyl-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-(4-trifluoromethylphenyl)-1,2,4-oxadiazol
-
-
5-[3-methyl-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-methyl-1,2,4-oxadiazole
-
-
5-[3-methyl-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-phenyl-1,2,4-oxadiazole
-
-
6-(7-nitro-2,1,3-benzoxadiazol-4-ylamino)hexanol
-
-
6-(7-nitro-2,1,3-benzoxadiazol-4-ylthio)hexanol
-
-
6-butanoyl-5,7-dihydroxy-4-phenyl-2H-chromen-2-one
-
a coumarin from Mammea africana, 23% total inhibition at 0.033 mM
7-nitro-2,1,3-benzoxadiazole derivatives
-
non-GSH peptidomimetic compounds, suicide inhibitors of the enzyme, binding structure and mechanism, overview, the compounds show strong GST inhibition and accumulation in tumor cells avoiding the extrusion mechanisms mediated by the multidrug resistance protein pumps
-
Al3+
-
68% inhibition at 100 mg/kg for male rats, 24% inhibition at 172.5 mg/kg for female rats
albendazol
-
17.87% inhibition at 1 mM
allyl-isothiocyanate
about 30% inhibition at 0.01 mM
alpha-endosulfan
-
about 55% residual activity at 0.1 mM
alpha-tocopherol
-
significant inhibition
ascorbate
-
ascorbate enhances the inhibitory effects of SH reagents, overview, inactivation of total cytosolic GST activity from liver by the oxygen radical-generating system Cu2+/ascorbate, two mechanisms: ROS-induced oxidation and non-specific Cu2+ binding to protein thiol groups
Atrazine
-
about 95% residual activity at 0.1 mM
benastatin A
-
IC50: 0.00041 mM
Berberine
complete inhibition at 0.1 mM
beta-endosulfan
-
about 90% residual activity at 0.1 mM
beta-ionone
about 15% inhibition at 0.1 mM
bifenthrin
-
7.27% inhibition of isoform GSTd10 at 0.05 mM
bile acid
-
41.78% inhibition at 1 mM
butanol
-
50% inactivation at 5%
Caffeine
about 25% inhibition at 0.01 mM
carbendazim
-
about 80% residual activity at 0.1 mM
carbosulfan
-
in vivo inhibition
chalcone
-
50% inhibition at 0.045 mM
chlorambucil
very poor inhibitor of the enzyme in contrast to ethacrynic acid
chrysin
about 30% inhibition at 0.1 mM
cinnamaldehyde
about 60% inhibition at 0.1 mM
citral
about 25% inhibition at 0.1 mM
Cl-
-
inhibits reaction with 1-chloro-2,4-dinitrobenzene with IC50: 0.12 mM. No inhibitory effect on the reaction with 7-chloro-4-nitrobenzo-2-oxa-1,3-diazole
clofentezine
-
28.05% inhibition of isoform GSTd14 at 0.05 mM and 27.68% inhibition of isoform GSTm09 at 0.05 mM
clothianidin
-
about 85% residual activity at 0.1 mM
coumarin
about 17% inhibition at 0.01 mM
Cr6+
-
58% inhibition at 10 mg/l
cumene hydroperoxide
-
2.5 mM, 43.3% inhibition of wild-type enzyme, 27% of mutant enzyme H144A, 50.6% of mutant enzyme V147A, 41.5% of mutant enzyme V147L, 48.1% of mutant enzyme R96A
cyclohexanone
about 3% inhibition at 0.1 mM
cypermethrin
-
in vivo inhibition
daidzein
-
inhibition of isozymes GST A1-1, M1-1, and P1-1
delphinidin chloride
-
strong inhibition
denatonium benzoate
about 10% inhibition at 0. 1 mM
desmedipham
-
about 62% residual activity at 0.1 mM
Dichloroacetic acid
O15217, O43708, O60760, P08263, P09210, P09211, P09488, P0CG30, P21266, P28161, P46439, P78417, Q03013, Q16772, Q7RTV2, Q9H4Y5 i.e. DC, used to treat lactic acidosis and has also been proposed as a novel anticancer agent is both a substrate and a mechanism-based inactivator of GSTZ1-1. Treatment with DCA progressively inactivates GSTZ1-1 and increases the elimination half-life of subsequent doses of DCA. recombinant GSTZ1*A protein is relatively resistant to DCA mediated inactivation when compared with the other isoforms
dieldrin
-
a potent reversible inhibitor toward hGSTA1-1, mixed-type inhibition, dieldrin binds specifically to the enzyme presumably at a position that partially overlaps with both the G- and H-site, a site distinct from binding of spiromesifen, binding structure overview
difheberan
-
about 47% residual activity at 0.1 mM
-
Diflubenzuron
-
about 45% residual activity at 0.1 mM
Digitonin
about 20% inhibition at 0.01 mM
Dimethyl sulfide
about 5% inhibition at 0.1 mM
dinitrophenyl-glutathione
-
-
DTT
-
50% inhibition at 10 mM
endosulfan
-
about 73% residual activity at 0.1 mM
epiandrosterone-aspartyl-glutathione
-
-
epiandrosterone-succinyl-glutathione
-
-
epichlorohydrin
-
3 mM, competitive
epiphyllocoumarin
95% inhibition at 0.1 mM
epoxiconazole
-
about 40% residual activity at 0.1 mM, complete inhibition at 0.2 mM
escin
about 10% inhibition at 0.1 mM
-
ethanol
-
inhibits the mu- and pi-class GST activities in vivo by 53% and 13%, respectively, in hepatocytes and the culture medium, the enzyme activity is increased in the cell medium, overview, the inhibitory effect is completely oe partially reversible by vitamin E or 4-methylpyrazole, respectively
ethyl 2-acrylamido-4-phenylthiazole-5-carboxylate
-
ethyl 2-acrylamido-4-phenylthiophene-3-carboxylate
-
ethyl 2-acrylamido-5-phenylthiophene-3-carboxylate
-
ethyl N-acryloyl-N-(4-phenylthiazol-2-yl)glycinate
-
fenamidone
-
about 78% residual activity at 0.1 mM
fenhexamid
-
about 85% residual activity at 0.1 mM
ferriprotoporphyrin IX
-
in presence of glutathione, GST serves as ligand for parasitotoxic ferriprotoporphyrin IX with a high- and a low-affinity binding site, uncompetitive inhibition type, overview
ferulic acid
-
inhibition of isozyme GST M1-1
fisetin
60% inhibition at 0.1 mM
flavonol
about 20% inhibition at 0.01 mM
fludioxonil
-
about 81% residual activity at 0.1 mM
fluopyram
-
about 82% residual activity at 0.1 mM
fluoxastrobin
-
about 75% residual activity at 0.1 mM
gamma-Glu-Cys(Acm)-Gly
85.2% remaining activity at 0.0003 mM
gamma-Glu-Cys(t-buthio)-Gly
85.6% remaining activity at 0.0003 mM
gamma-Glu-Met-Gly
79.4% remaining activity at 0.0003 mM
gamma-Glu-Thi-Gly
67.4% remaining activity at 0.0003 mM
gamma-glutamyl-(c-methoxycarbonyl)-alpha-glutamylglycine
-
-
gamma-glutamyl-5-azanylidyne-L-norvalylglycine
-
-
gamma-glutamyl-L-threonylglycine
-
-
gamma-L-glutamyl-L-seryl-glycine
-
-
genistein
-
inhibition of isozymes GST M1-1 and M2-2
geraniol
about 3% inhibition at 0.1 mM
geranyl acetate
about 5% inhibition at 0.01 mM
geshoidin
85% inhibition at 0.1 mM
Gly-Cys-Hyp
87.4% remaining activity at 0.0003 mM
GSSG
-
IC50: 2.0 mM for homodimeric enzyme, IC50: 2.6 mM for heterodimeric enzyme
hexanoic acid
about 5% inhibition at 0.1 mM
hexythiazox
-
11.21% inhibition of isoform GSTd14 at 0.05 mM and 12.94% inhibition of isoform GSTm09 at 0.05 mM
Hyp-Cys-Ala
98.7% remaining activity at 0.0003 mM
iodoacetamide
-
IC50: 40 mM for homodimeric enzyme, 8.7 mM for heterodimeric enzyme
iprodione
-
about 60% residual activity at 0.1 mM
K+
-
93.7% residual activity at 5 mM
KCl
-
IC50: 0.33 M for homodimeric enzyme, IC50: 0.18 M for heterodimeric enzyme
knipholone anthrone
95% inhibition at 0.1 mM
kresoxim-methyl
-
about 87% residual activity at 0.1 mM
L-g-glutamyl-S-[3-([5-[(5-[[5-([5-[(2-carbamimidamidoethyl)carbamoyl]-1-methyl-1H-pyrrol-3-yl]carbamoyl)-1-methyl-1H-pyrrol-3-yl]carbamoyl]-1-methyl-1H-pyrrol-3-yl)carbamoyl]-1-methyl-1H-pyrrol-3-yl]amino)-2-hydroxy-3-oxopropyl]-L-cysteinylglycine
-
a brostallicin derivative, inhibits GSTP1-1 and GSTM2-2
L-g-glutamyl-S-[3-([5-[(5-[[5-([5-[(2-carbamimidamidoethyl)carbamoyl]-1-methyl-1H-pyrrol-3-yl]carbamoyl)-1-methyl-1H-pyrrol-3-yl]carbamoyl]-1-methyl-1H-pyrrol-3-yl)carbamoyl]-1-methyl-1H-pyrrol-3-yl]amino)-3-oxo-2-(phosphonooxy)propyl]-L-cysteinylglycine
-
a brostallicin derivative, inhibits GSTP1-1 and GSTM2-2
L-gamma-glutamyl-S-(2-hydroxy-5-nitrophenyl)-L-cysteinylglycine
-
nonenzymatically synthesized GSH conjugate
L-gamma-glutamyl-S-[(17beta)-17-hydroxy-17-methyl-3-oxoandrost-4-en-4-yl]-L-cysteinylglycine
-
nonenzymatically synthesized GSH conjugate
L-gamma-glutamyl-S-[1-(3-chlorophenyl)-2-hydroxyethyl]-L-cysteinylglycine
-
nonenzymatically synthesized GSH conjugate
L-gamma-glutamyl-S-[2-(4-nitrophenyl)-2-oxoethyl]-L-cysteinylglycine
-
nonenzymatically synthesized GSH conjugate
L-gamma-glutamyl-S-[2-(6-oxocyclohex-1-en-1-yl)ethyl]-L-cysteinylglycine
-
nonenzymatically synthesized GSH conjugate
L-gamma-glutamyl-S-[3-[4-(carboxymethoxy)-2,3-dichlorophenyl]-3-oxopropyl]-L-cysteinylglycine
-
nonenzymatically synthesized GSH conjugate
limonene oxide
about 70% inhibition at 0.1 mM
lithocholate
-
50% inhibition at 0.1 mM
luteolin
about 16% inhibition at 0.01 mM
mercury acetate
-
50% inhibition at 28 nM
mesityl oxide
about 5% inhibition at 0.1 mM
metalaxyl
-
about 61% residual activity at 0.1 mM
methyl (E)-4-((4-chloro-3-(N,N-dimethylsulfamoyl)phenyl)-amino)but-2-enoate
-
methyl N-acryloyl-N-(4-phenylthiazol-2-yl)glycinate
-
N-((1E)-[4-(dimethylamino)phenyl]methylene)-2-([(1-methyl-1H-pyrrol-2-yl)sulfonyl]methyl)aniline
-
78.9% inhibition at 0.1 mM
N-((3-methylisoxazol-5-yl )methyl)-N-(4-(4-chloro-2-hydroxylphenyl)thiazol-2-yl)acrylamide
-
N-((3-methylisoxazol-5-yl)methyl)-N-(4-(2-hydroxylphenyl)-thiazol-2-yl)acrylamide
-
N-((3-methylisoxazol-5-yl)methyl)-N-(4-(2-methoxyphenyl)-thiazol-2-yl)acrylamide
-
N-((3-methylisoxazol-5-yl)methyl)-N-(4-(4-fluoro-2-hydroxylphenyl)thiazol-2-yl)acrylamide
-
N-((3-methylisoxazol-5-yl)methyl)-N-(4-(4-trifluoromethylphenyl)thiazol-2-yl)acrylamide
-
N-((3-methylisoxazol-5-yl)methyl)-N-(4-phenylthiazol-2-yl)-acrylamide
-
N-(1-benzyl-1H-pyrazol-4-yl)acrylamide
-
N-(1-phenyl-1H-pyrazol-4-yl)acrylamide
-
N-(2-((2-morpholinoethyl)amino)-2-oxoethyl)-N-(4-phenylthiazol-2-yl)acrylamide
-
N-(2-(cyclohexylamino)-2-oxoethyl)-N-(4-phenylthiazol-2-yl)-acrylamide
-
N-(2-(oxetan-3-ylamino)-2-oxoethyl)-N-(4-phenylthiazol-2-yl)-acrylamide
-
N-(2-morpholino-2-oxoethyl)-N-(4-phenylthiazol-2-yl)-acrylamide
-
N-(4-(2-chlorophenyl)thiazol-2-yl)acrylamide
-
N-(4-(2-fluorophenyl)thiazol-2-yl)acrylamide
-
N-(4-(2-hydroxylphenyl)thiazol-2-yl)acrylamide
-
N-(4-(2-hydroxyphenyl)thiophen-2-yl)-N-((3-methylisoxazol-5-yl)methyl)acrylamide
-
N-(4-(2-methoxyphenyl)thiazol-2-yl)acrylamide
-
N-(4-(3,4-dioxylphenyl)thiazol-2-yl)acrylamide
-
N-(4-(3-chlorophenyl)thiazol-2-yl)acrylamide
-
N-(4-(4-chlorophenyl)thiazol-2-yl)acrylamide
-
N-(4-(4-hydroxylphenyl)thiazol-2-yl)acrylamide
-
N-(4-(4-methoxyphenyl)thiazol-2-yl)acrylamide
-
N-(4-(4-methylphenyl)thiazol-2-yl)acrylamide
-
N-(4-(4-trifluoromethylphenyl)thiazol-2-yl)acrylamide
-
N-(4-(naphthalen-2-yl)thiazol-2-yl)acrylamide
-
N-(4-bromo-3-(N,N-dimethylsulfamoyl)phenyl)-2-chloroacetamide
-
-
N-(4-chloro-3-(N,N-dimethylsulfamoyl)phenyl)-2-cyanoacetamide
-
-
N-(4-chloro-3-(N,N-dimethylsulfamoyl)phenyl)-2-fluoroacetamide
-
-
N-(4-chloro-3-(N,N-dimethylsulfamoyl)phenyl)-2-oxopropanamide
-
-
N-(4-chloro-3-(N,N-dimethylsulfamoyl)phenyl)acrylamide
N-(4-phenyl-5-methyl-thiazol-2-yl)acrylamide
-
N-(4-phenylthiazol-2-yl)-N-(pyridin-3-ylmethyl)acrylamide
-
N-(4-phenylthiazol-2-yl)acrylamide
-
N-(5-phenylthiazol-2-yl)acrylamide
-
N-acetyl-p-benzoquinoneimine
concentration-dependent inhibition
N-acryloyl-N-(4-phenylthiazol-2-yl)glycine
-
N-benzyl-N-(4-phenylthiazol-2-yl)acrylamide
-
N-[(1E)-(2-chlorophenyl)methylene]-2-([(1-methyl-1H-pyrrol-2-yl)sulfonyl]methyl)aniline
-
88.8% inhibition at 0.1 mM
N-[(1E)-(4-chlorophenyl)methylene]-2-([(1-methyl-1H-pyrrol-2-yl)sulfonyl]methyl)aniline
-
60.4% inhibition at 0.1 mM
N-[(1E)-(4-fluorophenyl)methylene]-2-([(1-methyl-1H-pyrrol-2-yl)sulfonyl]methyl)aniline
-
37.1% inhibition at 0.1 mM
N-[(1E)-(5-bromo-2-methoxyphenyl)methylene]-2-([(1-methyl-1H-pyrrol-2-yl)sulfonyl]methyl)aniline
-
646% inhibition at 0.1 mM
N-[3-[(chloroacetyl)(4-nitrophenyl)amino]propyl]-2,2,2-trifluoroacetamide
i.e. ML175
N1-(4-chloro-3-(N,N-dimethylsulfamoyl)phenyl)oxalamide
-
-
N5-[(1S)-2-[(carboxymethyl)amino]-1-(cyanomethyl)-2-oxoethyl]glutamine
-
-
Na+
-
81.7% residual activity at 5 mM
naphthalene oxide
-
0.09 mM, competitive
naringenin
42% inhibition at 0.1 mM
naringin
about 17% inhibition at 0.01 mM
NH4Cl
-
IC50: 0.2 M for homodimeric enzyme, IC50: 0.12 M for heterodimeric enzyme
Nicotine
about 16% inhibition at 0.01 mM
p-nitrobenzylglutathione
-
papaverine
about 5% inhibition at 0.1 mM
paraxanthine
about 9% inhibition at 0.01 mM
pGlu-Cys(Trt)-Gly
82.3% remaining activity at 0.0003 mM
phenethyl-isothiocyanate
about 25% inhibition at 0.01 mM
phenmedipham
-
about 63% residual activity at 0.1 mM
phoxim
-
56% inhibition of isoform GST-1 at 0.1 mM, 14.8% inhibition of isoform GST-2 at 0.1 mM, 20.6% inhibition of isoform GST-3 at 0.1 mM
picoxystrobin
-
about 58% residual activity at 0.1 mM
piperidine
about 15% inhibition at 0.1 mM
piroxamine
-
about 92% residual activity at 0.1 mM
prasterone-aspartyl-glutathione
-
-
prasterone-succinyl-glutathione
-
-
prinoidin
70% inhibition at 0.1 mM
propyl-isothiocyanate
42% inhibition at 0.01 mM
Prostaglandins
-
isozyme GST P1-1 forms covalent complexes with cyclopentenone prostaglandins, i.e. cyPG 15-deoxy-DELTA12,14-PGJ2 and biotinylated 15d-PGJ2, mass spectrometry analysis, overview, irreversible inhibition
-
prothioconazol
-
about 85% residual activity at 0.1 mM
pyraclostrobin
-
about 70% residual activity at 0.1 mM
pyridaben
-
25.84% inhibition of isoform GSTm09 at 0.05 mM
Pyridine
about 17% inhibition at 0.1 mM
pyrimethanil
-
about 80% residual activity at 0.1 mM
Quinine
about 18% inhibition at 0.1 mM
resveratrol
-
inhibition of isozymes GST A2-2, M1-1, M2-2, and P1-1
S-(2,4-dinitrophenyl)glutathione
S-(2,4-dinitrophenyl)GSH
-
-
S-(4-azidophenacryl)-glutathione
-
competitive inhibitor, 27% loss of activity after 5 min
S-(4-Bromobenzyl)glutathione
S-(p-nitrobenzyl)-glutathione
-
-
S-carvone
S-carvone inhibits 26% of the enzyme activity at 0.01 mM and 84% at 0.1 mM
S-glutathionyl-phenylacetophenone
-
S-glutationyl-thiodione
-
S-hexyl-GSH
-
IC50: 0.0152 mM
S-Methylglutathione
-
competitive
S-phenylacetylglutathione
-
Sb3+
-
69% inhibition at 0.1 mM
SeO32-
-
20% inhibition at 0.1 mg/l
sinigrin hydrate
about 28% inhibition at 0.01 mM
Sodium dodecyl sulfate
-
denaturates irreversibly at 0.03 M
sodium oxide
-
about 50% residual activity at 0.1 mM
-
spiromesifen
-
a potent reversible inhibitor toward hGSTA1-1, mixed-type inhibition, spiromesifen binds specifically to the enzyme presumably at a position that partially overlaps with both the G- and H-site, a site distinct from binding of dieldrin, binding structure overview
strychnine
about 37% inhibition at 0.01 mM
superoxide anion
-
generated by a Fe3+/ascorbate system, inhibits cytosolic GSTs and microsomal GSTs by 30% and 65%, respectively. Addition of 2 mM DTT fails to completely reverse microsomal GST inhibition elicited by Fe3+/ascorbate, recovering only about 10% of this activity, but it completely reverses the inhibitory effect of Fe3+/ascorbate on cytosolic GST activity
tangeretin
complete inhibition at 0.1 mM
taurine
about 19% inhibition at 0.1 mM
teflubenzuron
-
about 62% residual activity at 0.1 mM
terbuthylazine
-
about 97% residual activity at 0.1 mM
tert-butyl N-acryloyl-N-(4-phenylthiazol-2-yl)glycinate
-
Theobromine
about 12% inhibition at 0.01 mM
theophylline
about 10% inhibition at 0.01 mM
thiamine hydrochloride
about 5% inhibition at 0.1 mM
thiazolidine
about 18% inhibition at 0.01 mM
Tic-Cys(Acm)-Gly
68.5% remaining activity at 0.0003 mM
Tic-Cys-Aib
80.1% remaining activity at 0.0003 mM
Tic-Cys-Sar
53% remaining activity at 0.0003 mM
tolclofos-methyl
-
about 55% residual activity at 0.1 mM
trans-2-hexen-1-al
about 23% inhibition at 0.1 mM
trans-2-nonenal
about 23% inhibition at 0.01 mM
trans-o-hydroxybenzylidene pyruvic acid
-
-
triadimenol
-
about 75% residual activity at 0.1 mM
trifloxystrobin
-
about 65% residual activity at 0.1 mM
triflumuron
-
about 70% residual activity at 0.1 mM
triphenylthin chloride
-
-
vinclozolin
-
about 73% residual activity at 0.1 mM
[(3aR,5R,7aR)-3a,5-dihydroxy-7a-methyloctahydro-1H-inden-1-one]-succinyl-glutathione
-
-
[(3aR,5S,7aR)-3a,5-dihydroxy-7a-methyloctahydro-1H-inden-1-one]-aspartyl-glutathione
-
-
[(3aR,5S,7aR)-3a,5-dihydroxy-7a-methyloctahydro-1H-inden-1-one]-succinyl-glutathione
-
-
1,4-pentadiene-3-one
-
curcumin derivative
1,4-pentadiene-3-one
-
curcumin derivative
1-Amino-4-{[4-({4-chloro-6-[(2-sulfophenyl)amino]-1,3,5-triazin-2-yl}amino)-3-sulfophenyl]amino}-9,10-dioxo-9,10-dihydro-2-anthracenesulfonic acid
-
1-Amino-4-{[4-({4-chloro-6-[(2-sulfophenyl)amino]-1,3,5-triazin-2-yl}amino)-3-sulfophenyl]amino}-9,10-dioxo-9,10-dihydro-2-anthracenesulfonic acid
-
1-Amino-4-{[4-({4-chloro-6-[(2-sulfophenyl)amino]-1,3,5-triazin-2-yl}amino)-3-sulfophenyl]amino}-9,10-dioxo-9,10-dihydro-2-anthracenesulfonic acid
-
1-Amino-4-{[4-({4-chloro-6-[(2-sulfophenyl)amino]-1,3,5-triazin-2-yl}amino)-3-sulfophenyl]amino}-9,10-dioxo-9,10-dihydro-2-anthracenesulfonic acid
Q8MU52
-
1-Amino-4-{[4-({4-chloro-6-[(2-sulfophenyl)amino]-1,3,5-triazin-2-yl}amino)-3-sulfophenyl]amino}-9,10-dioxo-9,10-dihydro-2-anthracenesulfonic acid
-
1-Amino-4-{[4-({4-chloro-6-[(2-sulfophenyl)amino]-1,3,5-triazin-2-yl}amino)-3-sulfophenyl]amino}-9,10-dioxo-9,10-dihydro-2-anthracenesulfonic acid
-
1-Amino-4-{[4-({4-chloro-6-[(2-sulfophenyl)amino]-1,3,5-triazin-2-yl}amino)-3-sulfophenyl]amino}-9,10-dioxo-9,10-dihydro-2-anthracenesulfonic acid
-
1-chloro-2,4-dinitrobenzene
-
competitive inhibition by the substrate
1-chloro-2,4-dinitrobenzene
-
-
2,5-dibenzylidenecyclopentanone
-
curcumin derivative
2,5-dibenzylidenecyclopentanone
-
curcumin derivative
2,6-dibenzylidenecyclohexanone
-
curcumin derivative
2,6-dibenzylidenecyclohexanone
-
curcumin derivative
2-chloro-N-[4-chloro-3-(N,N-dimethylsulfamoyl)phenyl]acetamide
i.e. C1-27
2-chloro-N-[4-chloro-3-(N,N-dimethylsulfamoyl)phenyl]acetamide
-
i.e. C1-27
4-nitrobenzyl chloride
-
1 mM, 50.5% inhibition of wild-type enzyme, 43.9% of mutant enzyme H144A, 40.8% of mutant enzyme V147A, 47.9% of mutant enzyme V147L, 30.8% of mutant enzyme R96A
4-nitrobenzyl chloride
-
50.8% inhibition of isoform GST-1 at 1 mM, 18.1% inhibition of isoform GST-2 at 1 mM, 33.3% inhibition of isoform GST-3 at 1 mM
4-[3-(5,5-dimethyl-4-oxo-4,5-dihydrofuran-2-yl)-3-hydroxybutoxy]-7H-furo[3,2-g]chromen-7-one
45% inhibition at 0.1 mM
4-[3-(5,5-dimethyl-4-oxo-4,5-dihydrofuran-2-yl)-3-hydroxybutoxy]-7H-furo[3,2-g]chromen-7-one
-
a furocoumarin from Dorstenia elliptica, 34% total inhibition at 0.033 mM
5,8-dihydroxy-1-(hydroxymethyl)naphtho[2,3-c]furan-4,9-dione
98.5% inhibition at 0.1 mM
5,8-dihydroxy-1-(hydroxymethyl)naphtho[2,3-c]furan-4,9-dione
-
an isofuranonaphthoquinone from Bulbine frutescens, the mode of inhibition is mixed, partial (G site) and noncompetitive (H site), 68% total inhibition at 0.033 mM
abamectin
-
17% inhibition of isoform GST-1 at 0.1 mM
abamectin
-
competitive inhibition (38.46% at 0.05 mM) of isoform GSTd14
Ag+
-
-
alachlor
-
about 90% residual activity at 0.1 mM
albendazole
-
50% inhibition at 0.52 mM
alizarin
-
50% inhibition at 0.0042 mM
As3+
-
48% inhibition at 0.5 mg/l
As3+
-
53% inhibition at 10 mg/kg
AsO42-
-
67% inhibition at 0.08 mM
-
AsO42-
-
80% inhibition at 0.05 mM
-
bendiocarb
-
-
bilirubin
-
50% inhibition at 0.009 mM
bilirubin
-
50% inhibition at 0.01-0.02 mM
bilirubin
-
no inhibitor, bilirubin binding site is different from catalytic site
bithionol
-
50% inhibition at 0.0077 mM
bromosulfophthalein
-
0.053 mM, 50% inhibition, isoenzyme I; 1.24 mM, 50% inhibition, isoenzyme II
bromosulfophthalein
-
50% inhibition at 0.001 mM
bromosulfophthalein
-
inhibits only minor form, but not major form
bromosulfophthalein
-
non-competitive inhibition
bromosulfophthalein
-
noncompetitive
bromosulfophthalein
noncompetitive inhibition
Bromosulphthalein
-
Ca2+
about 90% residual activity at 5 mM
Ca2+
-
91.3% residual activity at 5 mM
cantharidic acid
-
-
Cd2+
-
-
Cd2+
-
about 40% inhibition at 0.03 mM
Cd2+
-
65% inhibition at 0.1 mM
Cd2+
complete inhibition at 5 mM
Cd2+
-
at concentrations of 0.06-0.09 mg/l
Cd2+
-
35% inhibition at 2.5 mg/kg
Cd2+
-
53% inhibition at 0.1 mM
Cd2+
binds in the GSH-binding site by coordination with Asp and Gln residues, molecular modeling, overview
Cd2+
-
90% inhibition at 1 mg/kg
Cd2+
-
50% inhibition at 0.05 mM
chlorfenapyr
-
-
chlorotriphenyltin
-
0.33 mM, 50% inhibition, isoenzyme I; 6.4 mM, 50% inhibition, isoenzyme II
chlorpyrifos
-
in vivo inhibition
Cibacron blue
-
Cibacron blue
-
0.053 mM, 50% inhibition, isoenzyme I; 0.073 mM, 50% inhibition, isoenzyme II
Cibacron blue
-
50% inhibition at 0.00009 mM
Cibacron blue
91% inhibition at 0.1 mM; 94% inhibition at 0.1 mM
Cibacron blue
-
IC50: 10 nM
Cibacron blue
94.3% inhibition at 0.064 mM
Cibacron blue
-
most potent inhibitor
Cibacron blue
-
significant inhibition
Cibacron blue
-
non-competitive inhibition
Cibacron blue
-
noncompetitive
Cibacron blue
Thermosynechococcus vestitus
-
Cibacron blue
-
IC50: 0.048 mM for homodimeric enzyme, IC50: 0.0084 mM for heterodimeric enzyme
Co2+
-
-
Cu2+
-
-
Cu2+
-
61% inhibition at 0.1 mM
Cu2+
complete inhibition at 5 mM
Cu2+
-
98.7% residual activity at 5 mM
Cu2+
-
about 40% inhibition at 0.005 mM
Cu2+
-
about 52% inhibition at 0.008 mM
Cu2+
-
37-45% inhibition at 100-800 mg/kg
Cu2+
-
inhibitory in either the absence or presence of ascorbate, inactivation of total cytosolic GST activity from liver by the oxygen radical-generating system Cu2+/ascorbate, two mechanisms: ROS-induced oxidation and non-specific Cu2+ binding to protein thiol groups, the inhibition is prevented by glutathione but not 1-chloro-2,4-dinitrobenzene, Cu2+ inhibition affects the Km for glutathione but not of 1-chloro-2,4-dinitrobenzene, overview
curcumin
-
inhibition of isozymes GST A1-1, A2-2, M1-1, M2-2, and P1-1
curcumin
-
a promising chemotherapeutic agent, inhibits human GSTA1-1, GSTM1-1, and GSTP1-1 isoenzymes
deltamethrin
-
0.01 mM, 65.4% inhibition of wild-type enzyme, 44.2% of mutant enzyme H144A, 59.5% of mutant enzyme V147A, 66.1% of mutant enzyme V147L, 88.6% of mutant enzyme R96A
deltamethrin
41% inhibition at 1 mM; 54% inhibition at 1 mM
deltamethrin
an insecticide
diazinon
-
about 30% residual activity at 1 mM
diazinon
-
in the presence of 1 mM diazinon, isoform GST7 shows 23% of its original activity , whereas the activity of isoform GST20 is decreased to about 50% of its original activity
dichlorvos
-
41.87% inhibition at 1.45 mM
dichlorvos
-
64.47% inhibition at 14.45 mM
dithiothreitol
-
32% residual activity at 10 mM
EDTA
-
-
EDTA
-
90% residual activity at 10 mM
ellagic acid
-
50% inhibition at 0.0006 mM
ellagic acid
-
inhibition of isozymes GST A1-1, A2-2, M1-1, M2-2, and P1-1, effects on substrate kinetics, overview
Ethacrynic acid
-
0.001 mM, 35.3% inhibition of wild-type enzyme, 32.7% of mutant enzyme H144A, 27.8% of mutant enzyme V147A, 23.0% of mutant enzyme V147L, 29.1% of mutant enzyme R96A
Ethacrynic acid
complete inhibition at 0.1 mM
Ethacrynic acid
-
less than 10% residual activity at 0.5 mM
Ethacrynic acid
-
88.6% inhibition at 0.02 mM
Ethacrynic acid
-
inhibits isozyme GSTP1-1
Ethacrynic acid
-
0.00028 mM
Ethacrynic acid
-
specific inhibition
Fe2+
about 30% residual activity at 5 mM
Fe2+
-
40% residual activity at 5 mM
fenitrothion
50% inhibition at 1 mM; 56% inhibition at 1 mM
fenitrothion
an insecticide
glutathione
-
competitive inhibition by the substrate
glutathione
-
a decrease in the activity of the enzyme is observed when glutathione concentration is increased beyond 1.0 mM
guanidine hydrochloride
retains 30% of its functionality at 0.5 M
guanidine hydrochloride
-
denaturation at 6 M
guanidine hydrochloride
-
reversible denaturation at 3.2 M
H2O2
-
inactivation of cytosolic GST activity from liver
H2O2
-
inhibits cytosolic GST by about 65% and activates microsomal GST to about 175%
H2O2
-
2.1% residual activity at 0.2% (v/v)
haematin
-
haematin
-
non-competitive inhibition
Hematin
-
0.13 mM, 50% inhibition, isoenzyme I; 1.81 mM, 50% inhibition, isoenzyme II
Hematin
-
non competitive with transferase activity
Hematin
binding by isozymes with high affinity
hemin
-
competitive with 1-chloro-2,4-dinitrobenzene, non-competitive with glutathione
hemin
-
noncompetitive, 86% inhibition at 0.0055 mM
Hexachlorophene
-
50% inhibition at 0.00034 mM
hexyl glutathione
-
-
hexyl glutathione
Thermosynechococcus vestitus
-
Hg2+
-
-
Hg2+
-
70% inhibition at 0.1 mM
Hg2+
complete inhibition at 5 mM
Hg2+
-
70% inhibition at 0.0009 mg/kg
imidacloprid
-
about 92% residual activity at 0.1 mM
imidacloprid
-
about 30% residual activity at 1 mM
Indocyanine green
-
-
Indocyanine green
-
inhibition of transferase B is greater than inhibition of transferase AA
indomethacin
-
-
indomethacin
-
uncompetitive inhibition
iodoacetate
-
weak
kaempferol
about 42% inhibition at 0.01 mM
kaempferol
-
inhibition of isozymes GST M1-1 and M2-2
lambda-cyhalothrin
-
-
Mg2+
about 81% residual activity at 5 mM
Mg2+
-
89.3% residual activity at 5 mM
Mn2+
about 95% residual activity at 5 mM
Mn2+
-
83.8% residual activity at 5 mM
N-(4-chloro-3-(N,N-dimethylsulfamoyl)phenyl)acrylamide
-
N-(4-chloro-3-(N,N-dimethylsulfamoyl)phenyl)acrylamide
-
-
N-ethylmaleimide
-
completely inhibits form IX and X at 20 mM after 30 min, but not forms I-VIII
N-ethylmaleimide
-
complete loss of activity after 30 min at 5 mM
NaCl
-
26.22% inhibition at 1 mM
NaCl
-
IC50: 0.332 M for homodimeric enzyme, IC50: 0.17 M for heterodimeric enzyme
NaCl
-
0.2 M, 50% inhibition
NEM
-
IC50: 33 mM
Ni2+
-
37% inhibition at 0.5 mM
paraoxon
-
80-72% inhibition at 1.541 M
paraoxon
-
49.51% inhibition at 154 mM
Pb2+
-
-
Pb2+
-
42% inhibition at 0.1 mM
Pb2+
-
77% inhibition at 0.02 mg/l in gills, 44% inhibition at 0.02 mg/l in digestive gland
Pb2+
complete inhibition at 5 mM
Pb2+
-
74% inhibition at 0.1 mM
Pb2+
-
45% inhibition at 0.05 mM
Pb2+
-
55% inhibition at 0.1% (w/v)
Pb2+
-
80% inhibition at 0.05 mM
permethrin
-
0.01 mM, 51.1% inhibition of wild-type enzyme, 38.8% of mutant enzyme H144A, 53.1% of mutant enzyme V147A, 49% of mutant enzyme V147L, 65.5% of mutant enzyme R96A
permethrin
24% inhibition at 1 mM; 33% inhibition at 1 mM
permethrin
-
about 45% residual activity at 0.1 mM
permethrin
-
35% inhibition of isoform GST-1 at 0.1 mM
permethrin
an insecticide
permethrin
-
about 50% residual activity at 1 mM
praziquantel
-
31.31% inhibition at 1 mM
protoporphyrin IX
-
50% inhibition at 0.03 mM
protoporphyrin IX
Q8MU52
-
protoporphyrin IX
31.3% to 85.6% inhibition at 0.00025 mM to 0.25 mM
quercetin
-
50% inhibition at 0.0006 mM
quercetin
complete inhibition at 0.1 mM, 52% inhibition at 0.01 mM
quercetin
-
inhibition of isozymes GST M1-1 and M2-2
quercetin
-
strong inhibition
Rose bengal
-
-
Rose bengal
-
non-competitive inhibition
Rose bengal
-
IC50: 0.00031 mM for homodimeric enzyme, IC50: 0.00047 mM for heterodimeric enzyme
S-(2,4-dinitrophenyl)glutathione
-
product inhibition
S-(2,4-dinitrophenyl)glutathione
-
IC50: 0.0034 mM
S-(2,4-dinitrophenyl)glutathione
-
-
S-(2,4-dinitrophenyl)glutathione
-
mixed-type inhibition by reaction product, complex inhibition pattern
S-(2,4-dinitrophenyl)glutathione
-
-
S-(4-Bromobenzyl)glutathione
-
-
S-(4-Bromobenzyl)glutathione
-
-
S-hexyl glutathione
-
0.01 mM, 21.7% inhibition of wild-type enzyme, 23% of mutant enzyme H144A, 10.8% of mutant enzyme V147A, 24.2% of mutant enzyme V147L, 14.7% of mutant enzyme R96A
S-hexyl-glutathione
binding structure with wild-type and mutant Y119E and F123A enzymes, overview
S-hexylglutathione
inhibitor binding does not induce significant conformational changes in the protein
S-hexylglutathione
binding structure, overview
S-hexylglutathione
-
IC50: 0.34 mM
S-hexylglutathione
-
binding structure, overview
S-hexylglutathione
-
IC50: 0.00031 mM for homodimeric enzyme, IC50: 0.00039 mM for heterodimeric enzyme
S-methyl-GSH
-
-
S-methyl-GSH
-
IC50: 0.0123 mM
SDS
-
-
SDS
-
61% residual activity at 10 mM
SDS
-
12.7% residual activity at 10 mM
sulfophthalein
-
-
Tannic acid
-
-
tributyltin
-
-
tributyltin
-
70% inhibition at 0.3 mg/kg
Tributyltin acetate
-
-
Triethyltin bromide
-
-
Triphenyltin
-
-
Triphenyltin chloride
-
50% inhibition at 0.0003 mM
Triphenyltin chloride
-
-
Triphenyltin chloride
-
-
Triphenyltin chloride
noncompetitive inhibition
Urea
-
-
Urea
Ilex sp.
-
25% inactivation at 0.7 M
Urea
-
denaturates at 7.2 M, reversible
Vanillin
-
Vanillin
less than 10% inhibition at 0.1 mM
Zn2+
-
-
Zn2+
about 1% residual activity at 5 mM
Zn2+
-
65.4% residual activity at 5 mM
additional information
not inhibited by haematin and N-ethylmaleimade
-
additional information
-
not inhibited by haematin and N-ethylmaleimade
-
additional information
the enzyme is completely resistant against insecticides fenitrothion, deltamethrin, and permethrin, in vivo toxicity, overview
-
additional information
the enzyme is completely resistant against insecticides fenitrothion, deltamethrin, and permethrin, in vivo toxicity, overview
-
additional information
the enzyme is completely resistant against insecticides fenitrothion, deltamethrin, and permethrin, in vivo toxicity, overview
-
additional information
-
the enzyme is completely resistant against insecticides fenitrothion, deltamethrin, and permethrin, in vivo toxicity, overview
-
additional information
-
not inhibited by spiroteramat, metribuzin and boscalid
-
additional information
-
no inhibition by diazinon up to 0.07 mg/l and by Cr6+ up to 0.00028 mg/l
-
additional information
-
isoforms GST-2 and GST-3 are not inhibited by permethrin and abamectin. Isoforms GST-1, GST-2, and GST3 are not inhibited by spinosad
-
additional information
-
no inhibition of the cytosolic isozyme by chenodeoxycholic acid and 4-nitropyridine-N-oxide
-
additional information
-
not inhibited by bromosulfophthalein
-
additional information
-
inhibitory potencies of chalcone derivatives on GSTP1-1, molecular modeling, overview. No or poor inhibition by I-02, I-03, I-10, I-13, I-14, I-15, and I-16
-
additional information
-
antitumor and antirpoliferative activities of inhibitors versus cancer cell lines, overview
-
additional information
-
construction of three series of curcumin derivatives, inhibitory potencies on GSt isozymes, overview
-
additional information
-
synthesis, screening, and potencies of 2-(pyrrolesulfonylmethyl)-N-arylimines as inhibitors of human glutathione transferase A1-1, in silico molecular docking analysis and molecular modeling, overview
-
additional information
-
hGSTA1-1 is more susceptible to inhibition by pesticides than other isoenzymes. In silico docking analysis and kinetic inhibition studies, overview
-
additional information
not inhibited by acetyl-gamma-Glu-Cys-Gly, gamma-Glu-Cys-Aib, gamma-Glu-Cys-a-t-butyl-Gly, Sar-Cys(Trt)-Gly, Tic-Cys-Ala, and gamma-Glu-NMeCys-Gly
-
additional information
-
not inhibited by acetyl-gamma-Glu-Cys-Gly, gamma-Glu-Cys-Aib, gamma-Glu-Cys-a-t-butyl-Gly, Sar-Cys(Trt)-Gly, Tic-Cys-Ala, and gamma-Glu-NMeCys-Gly
-
additional information
-
the three populations of Liposcelis paeta show different susceptibilities to different insecticides, even after they are reared on diets consisting of 25% ethacrynic acid, no inhibition by Ba2+
-
additional information
-
difference in sensitivity to inhibition of enzyme MI, MII and MIII
-
additional information
-
structural and mechanistic studies on ligand binding and enzyme inhibition, overview
-
additional information
presence of salts effectively inhibits PvGST enzymatic activity by quenching the nucleophilicity of the thiolate anion of GSH, relative decrease in descending order MgCl2, MgSO4, NaCl, Na2SO4
-
additional information
-
presence of salts effectively inhibits PvGST enzymatic activity by quenching the nucleophilicity of the thiolate anion of GSH, relative decrease in descending order MgCl2, MgSO4, NaCl, Na2SO4
-
additional information
-
of seven major rat isoenzymes
-
additional information
-
presence of superoxide dismutase and catalase reduces the activity of the microsomal GST isozyme, but only catalase can reduce the activity of the cytosolic GST
-
additional information
-
construction of three series of curcumin derivatives, inhibitory potencies on GSt isozymes, overview
-
additional information
-
no inhibition by EGTA and deferoxamine
-
additional information
not inhibited by 6-methyl-5-hepten-2-one
-
additional information
-
not inhibited by 18alpha-glycyrrhetinic acid and cyanidin
-
additional information
-
implementation of both structure-based drug design and the concept of polyvalency to discover a series of potent and unsymmetrical GST inhibitors, stoichiometry of one inhibitor molecule per GST monomer via isothermal titration calorimetric measurement, overview, molecular modeling
-
additional information
-
cantharidin has no effect on isoform SGSTalpha1 activity
-
additional information
bulky compounds with two aromatic rings, e.g. phenylurea-based insecticides, behave as strong inhibitors showing inhibition between 75% and 94%
-
additional information
-
bulky compounds with two aromatic rings, e.g. phenylurea-based insecticides, behave as strong inhibitors showing inhibition between 75% and 94%
-