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1,2-Dihydroxybenzene 3,5-disulfonic acid
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1-(2-Thenoyl)-3,3,3-trifluoroacetone
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2,2-dimethyl-5-nitro-2H-benzimidazole
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2-[(7-nitro-3-oxo-2,1,3l5-benzoxadiazol-4-yl)oxy]phenol
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2-[(E)-(4-hydroxyphenyl)diazenyl]-1-benzothiophene-3-ol
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4-(4-chloroanilino)-4-oxobutanoic acid
4-(4-methylanilino)-4-oxobutanoic acid
4-(hexylamino)-4-oxobutanoic acid
4-[3-(1H-benzimidazol-2-yl)anilino]-4-oxobutanoic acid
4-[4-(1,3-benzothiazol-2-yl)anilino]-4-oxobutanoic acid
4-[4-(1,3-benzoxazol-2-yl)anilino]-4-oxobutanoic acid
4-[4-(1H-benzimidazol-2-yl)anilino]-4-oxobutanoic acid
4-[4-(1H-naphtho[2,3-d]imidazol-2-yl)anilino]-4-oxobutanoic acid
4-[4-(5-methyl-1H-benzimidazol-2-yl)anilino]-4-oxobutanoic acid
4-[4-[5-(3-carboxypropanamido)-1H-benzimidazol-2-yl]anilino]-4-oxobutanoic acid
4-[4-[5-(cyclohexa-2,4-diene-1-carbonyl)-1H-benzimidazol-2-yl]anilino]-4-oxobutanoic acid
5-[(E)-(3-chlorophenyl)diazenyl]-2-hydroxybenzaldehyde
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6-(7-nitro-2,1,3-benzoxadiazol-4-ylthio)hexanol
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adriamycin
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significant inhibition of reaction with hydrophobic electron acceptors, coenzyme Q or vitamin K3
alpha-tocopheryl succinate
Cetylpyridinium bromide
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Chloroquine
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inhibits reaction with coenzyme Q1, no inhibition of the reaction with 2,6-dichloroindophenol
Cu2+
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specifically inhibits phenazine methosulfate coupled 3-(4,5-dimethylthiazolyl-2)-2,5-diphenyltetrazolium bromide reduction assay
D-2-Phosphoglyceric acid
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D-glyceraldehyde 3-phosphate
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Digitonin
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strong inhibition, the activity is recovered to 148% of control values by the addition of exogenous synthetic analog of CoQ idebenone, i.e. hydroxydecylubiquinone, and cytochrome c. The compound also strongly activates glycerol-3-phosphate oxidation inhibited by endogenous or added free fatty acids
dihydroxyacetone phosphate
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ethyl 4-(3-oxo-1,2-thiazol-2(3H)-yl)benzoate
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FMN
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reaction with methylene blue
glyceraldehyde 3-phosphate
glyceraldehyde-3-phosphate
competitive inhibitor
glyceric acid 2-phosphate
competitive inhibitor
L-Glyceraldehyde 3-phosphate
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methyl 4-(4-methylanilino)-4-oxobutanoate
N-(3,5-dibromo-4-hydroxyphenyl)-4-methylbenzene-1-sulfonamide
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N-[4-(1H-naphtho[2,3-d]imidazol-2-yl)phenyl]butanamide
N-[4-(5,6-dihydro-1H-benzimidazol-2-yl)phenyl]-2-oxopropanamide
N-[4-(5,6-dihydro-1H-benzimidazol-2-yl)phenyl]-3-methylbutanamide
N-[4-(5,6-dihydro-1H-benzimidazol-2-yl)phenyl]-4-ethoxybenzamide
N-[4-(5,6-dihydro-1H-benzimidazol-2-yl)phenyl]cyclopropanecarboxamide
N-[4-(5,6-dihydro-1H-benzimidazol-2-yl)phenyl]furan-2-carboxamide
Thenoyltrifluoroacetone
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1,10-phenanthroline
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4-(4-chloroanilino)-4-oxobutanoic acid
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4-(4-chloroanilino)-4-oxobutanoic acid
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4-(4-methylanilino)-4-oxobutanoic acid
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4-(4-methylanilino)-4-oxobutanoic acid
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4-(hexylamino)-4-oxobutanoic acid
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4-(hexylamino)-4-oxobutanoic acid
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4-[3-(1H-benzimidazol-2-yl)anilino]-4-oxobutanoic acid
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4-[3-(1H-benzimidazol-2-yl)anilino]-4-oxobutanoic acid
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4-[4-(1,3-benzothiazol-2-yl)anilino]-4-oxobutanoic acid
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4-[4-(1,3-benzothiazol-2-yl)anilino]-4-oxobutanoic acid
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4-[4-(1,3-benzoxazol-2-yl)anilino]-4-oxobutanoic acid
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4-[4-(1,3-benzoxazol-2-yl)anilino]-4-oxobutanoic acid
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4-[4-(1H-benzimidazol-2-yl)anilino]-4-oxobutanoic acid
mixed type inhibition, potent and selective inhibitor
4-[4-(1H-benzimidazol-2-yl)anilino]-4-oxobutanoic acid
mixed type inhibition, potent and selective inhibitor
4-[4-(1H-naphtho[2,3-d]imidazol-2-yl)anilino]-4-oxobutanoic acid
mixed type inhibition
4-[4-(1H-naphtho[2,3-d]imidazol-2-yl)anilino]-4-oxobutanoic acid
mixed type inhibition
4-[4-(5-methyl-1H-benzimidazol-2-yl)anilino]-4-oxobutanoic acid
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4-[4-(5-methyl-1H-benzimidazol-2-yl)anilino]-4-oxobutanoic acid
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4-[4-[5-(3-carboxypropanamido)-1H-benzimidazol-2-yl]anilino]-4-oxobutanoic acid
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4-[4-[5-(3-carboxypropanamido)-1H-benzimidazol-2-yl]anilino]-4-oxobutanoic acid
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4-[4-[5-(cyclohexa-2,4-diene-1-carbonyl)-1H-benzimidazol-2-yl]anilino]-4-oxobutanoic acid
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4-[4-[5-(cyclohexa-2,4-diene-1-carbonyl)-1H-benzimidazol-2-yl]anilino]-4-oxobutanoic acid
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alpha-tocopheryl succinate
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alpha-tocopheryl succinate
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D-3-phosphoglyceric acid
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D-3-phosphoglyceric acid
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D-3-phosphoglyceric acid
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competitive with respect to glycerophosphate
glyceraldehyde 3-phosphate
about 80% inhibition at 2.5 mM, glyceraldehyde 3-phosphate is not a specific inhibitor of mGPDH but also alters succinate oxidation
glyceraldehyde 3-phosphate
about 80% inhibition at 2.5 mM, glyceraldehyde 3-phosphate is not a specific inhibitor of mGPDH but also alters succinate oxidation
glyceraldehyde 3-phosphate
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D-3-glyceraldehyde phosphate; L-3-glyceraldehyde phosphate
glyceraldehyde 3-phosphate
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glycerone phosphate
product inhibition
glycerone phosphate
product inhibition
methyl 4-(4-methylanilino)-4-oxobutanoate
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methyl 4-(4-methylanilino)-4-oxobutanoate
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N-[4-(1H-naphtho[2,3-d]imidazol-2-yl)phenyl]butanamide
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N-[4-(1H-naphtho[2,3-d]imidazol-2-yl)phenyl]butanamide
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N-[4-(5,6-dihydro-1H-benzimidazol-2-yl)phenyl]-2-oxopropanamide
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N-[4-(5,6-dihydro-1H-benzimidazol-2-yl)phenyl]-2-oxopropanamide
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N-[4-(5,6-dihydro-1H-benzimidazol-2-yl)phenyl]-3-methylbutanamide
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N-[4-(5,6-dihydro-1H-benzimidazol-2-yl)phenyl]-3-methylbutanamide
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N-[4-(5,6-dihydro-1H-benzimidazol-2-yl)phenyl]-4-ethoxybenzamide
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N-[4-(5,6-dihydro-1H-benzimidazol-2-yl)phenyl]-4-ethoxybenzamide
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N-[4-(5,6-dihydro-1H-benzimidazol-2-yl)phenyl]cyclopropanecarboxamide
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N-[4-(5,6-dihydro-1H-benzimidazol-2-yl)phenyl]cyclopropanecarboxamide
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N-[4-(5,6-dihydro-1H-benzimidazol-2-yl)phenyl]furan-2-carboxamide
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N-[4-(5,6-dihydro-1H-benzimidazol-2-yl)phenyl]furan-2-carboxamide
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PCMB
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phosphoenolpyruvate
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phosphoenolpyruvate
competitive inhibitor
Triton X100
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Triton X100
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in presence of phospholipids
Zn2+
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specifically inhibits ferricyanide reduction assay
additional information
screening and identification of cell-permeant small-molecule inhibitors of mGPDH (iGP) discovered through small-molecule screening. Structure-activity analysis identifies a core benzimidazole-phenyl-succinamide structure as being essential to inhibition of mGPDH while modifications to the benzimidazole ring system modulate both potency and off-target effects. The iGPs penetrate cellular membranes. Inhibitor selectivity, and effects of the inhibitors on kinetics of mGPDH, overview
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additional information
screening and identification of cell-permeant small-molecule inhibitors of mGPDH (iGP) discovered through small-molecule screening. Structure-activity analysis identifies a core benzimidazole-phenyl-succinamide structure as being essential to inhibition of mGPDH while modifications to the benzimidazole ring system modulate both potency and off-target effects. The iGPs penetrate cellular membranes. Inhibitor selectivity, and effects of the inhibitors on kinetics of mGPDH, overview
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