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(2-chlorophenyl)(dimethoxyphosphoryl)methyl [3-(trifluoromethyl)phenoxy]acetate
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(3,4-dichlorophenyl)(dimethoxyphosphoryl)methyl [3-(trifluoromethyl)phenoxy]acetate
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(3-chlorophenyl)(dimethoxyphosphoryl)methyl [3-(trifluoromethyl)phenoxy]acetate
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(4-chlorophenyl)(dimethoxyphosphoryl)methyl [3-(trifluoromethyl)phenoxy]acetate
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(dimethoxyphosphoryl)(4-methylphenyl)methyl [3-(trifluoromethyl)phenoxy]acetate
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(dimethoxyphosphoryl)(phenyl)methyl (2,3-dichlorophenoxy)acetate
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(dimethoxyphosphoryl)(phenyl)methyl (2,6-dichlorophenoxy)acetate
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(dimethoxyphosphoryl)(phenyl)methyl (2-chloro-5-methylphenoxy)acetate
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(dimethoxyphosphoryl)(phenyl)methyl (3-fluorophenoxy)acetate
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(dimethoxyphosphoryl)(phenyl)methyl (4-chloro-2-methylphenoxy)acetate
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(dimethoxyphosphoryl)(phenyl)methyl (4-chloro-3-methylphenoxy)acetate
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(dimethoxyphosphoryl)(phenyl)methyl (4-chlorophenoxy)acetate
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(dimethoxyphosphoryl)(phenyl)methyl (4-fluorophenoxy)acetate
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1-(dimethoxyphosphoryl)ethyl (2,3-dichlorophenoxy)acetate
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1-(dimethoxyphosphoryl)ethyl (2,6-dichlorophenoxy)acetate
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1-(dimethoxyphosphoryl)ethyl (2-chloro-5-methylphenoxy)acetate
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1-(dimethoxyphosphoryl)ethyl (3-fluorophenoxy)acetate
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1-(dimethoxyphosphoryl)ethyl (4-chloro-2-methylphenoxy)acetate
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1-(dimethoxyphosphoryl)ethyl (4-chloro-3-methylphenoxy)acetate
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1-(dimethoxyphosphoryl)ethyl (4-chlorophenoxy)acetate
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1-(dimethoxyphosphoryl)ethyl (4-fluorophenoxy)acetate
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2,2'-Dithiopyridine
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1.1 mM, 30% inhibition
2,2,2-trichloro-1-(dimethoxyphosphoryl)ethyl (2,3-dichlorophenoxy)acetate
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2,2,2-trichloro-1-(dimethoxyphosphoryl)ethyl (2-chloro-5-methylphenoxy)acetate
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2,2,2-trichloro-1-(dimethoxyphosphoryl)ethyl (3-fluorophenoxy)acetate
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2,2,2-trichloro-1-(dimethoxyphosphoryl)ethyl (4-chloro-2-methylphenoxy)acetate
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2,2,2-trichloro-1-(dimethoxyphosphoryl)ethyl (4-chloro-3-methylphenoxy)acetate
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2,2,2-trichloro-1-(dimethoxyphosphoryl)ethyl (4-chlorophenoxy)acetate
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2,2,2-trichloro-1-(dimethoxyphosphoryl)ethyl (4-fluorophenoxy)acetate
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3-Bromopyruvate
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suicide substrate
3-deazathiamine diphosphate
4-((1-((4-amino-2-methylpyrimidin-5-yl)methyl)-5-iodo-1H-1,2,3-triazol-4-yl)methoxy)benzonitrile
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exhibits very good enzyme-selective inhibition of PDH-E1 between pig heart and Escherichia coli and activity against Rhizoctonia solani and Botrytis cinerea even at 12.5 lg/ml
5,5'-dithiobis(2-nitrobenzoate)
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1.1 mM, 35% inhibition
5-((4-((4-bromophenoxy)methyl)-5-iodo-1H-1,2,3-triazol-1-yl)methyl)-2-methylpyrimidin-4-amine
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exhibits activity against Rhizoctonia solani and Botrytis cinerea even at 12.5 lg/ml
5-((4-((4-chloro-3-methylphenoxy)methyl)-5-iodo-1H-1,2,3-triazol-1-yl)methyl)-2-methylpyrimidin-4-amine
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5-((4-((4-chlorophenoxy)methyl)-5-iodo-1H-1,2,3-triazol-1-yl)methyl)-2-methylpyrimidin-4-amine
acetyl-CoA
product inhibition, acetyl CoA interacts directly with the E1p component
AgNO3
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18 mol per mol enzyme, complete inhibition
Aluminium sulfate
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1.1 mM, 35% inhibition
Ba2+
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0.11 mM, 10% inhibition
Cd2+
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0.032 mM, complete inhibition
citrate
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noncompetitive inhibition
CoA
allosteric inhibition
Cu2+
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0.36 mM, complete inhibition
CuSO4
EC50 value against Synechocystis sp. PCC 6803 is 0.002 mM
D-glucose
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treatment of cardiac fibroblasts with 35 mM D-glucose for 72 h reduces the PDH activity remarkably. 0.2 mM thiamine dramatically recovers the high glucose-induced PDH inhibition
EDTA
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0.036 mM, 40% inhibition, 0.36 mM, complete inhibition, reversed by addition of excess Mg2+ and Ca2+
Fluoropyruvate
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competitive with respect to pyruvate, both free and complex bound enzyme behave in the same manner
KCl
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at 2 M, 50% residual activity of enzyme expressed in Escherichia coli
methyl acetylphosphonate
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phosphonate analogue of pyruvate, leading to formation of a stable 1,4-imino-2-alpha-phosphonolactyl-thiamindiphosphate
Methylacetylphosphonate
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MgATP2-
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due to phosphorylation of the enzyme by pyruvate dehydrogenase kinase
N-((1-((4-amino-2-methylpyrimidin-5-yl)methyl)-1H-1,2,3-triazol-4-yl) methyl)-2,4,6-trimethylbenzenesulfonamide
thiamim diphosphate analogue, EC50 value against Synechocystis sp. PCC 6803 is 0.0043 mM
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N-((1-((4-amino-2-methylpyrimidin-5-yl)methyl)-1H-1,2,3-triazol-4-yl) methyl)-2-nitrobenzenesulfonamide
thiamim diphosphate analogue, EC50 value against Synechocystis sp. PCC 6803 is 0.0063 mM
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N-((1-((4-amino-2-methylpyrimidin-5-yl)methyl)-1H-1,2,3-triazol-4-yl) methyl)-4-bromobenzenesulfonamide
thiamin diphosphate analogue, EC50 value against Synechocystis sp. PCC 6803 is 0.009 mM
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N-((1-((4-amino-2-methylpyrimidin-5-yl)methyl)-5-iodo-1H-1,2,3-triazol-4-yl) methyl)-4-chlorobenzenesulfonamide
thiamim diphosphate analogue, EC50 value against Synechocystis sp. PCC 6803 is 0.0018 mM
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N-((1-((4-amino-2-methylpyrimidin-5-yl)methyl)-5-iodo-1H-1,2,3-triazol-4-yl)methyl)-2,4,6-trimethylbenzenesulfonamide
thiamim diphosphate analogue, EC50 value against Synechocystis sp. PCC 6803 is 0.002 mM
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N-((1-((4-amino-2-methylpyrimidin-5-yl)methyl)-5-iodo-1H-1,2,3-triazol-4-yl)methyl)-4-bromobenzenesulfonamide
thiamim diphosphate analogue, EC50 value against Synechocystis sp. PCC 6803 is 0.002 mM
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N-((1-((4-amino-2-methylpyrimidin-5-yl)methyl)-5-iodo-1H-1,2,3-triazol-4-yl)methyl)-4-fluorobenzenesulfonamide
thiamim diphosphate analogue, EC50 value against Synechocystis sp. PCC 6803 is 0.0017 mM
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N-((1-((4-amino-2-methylpyrimidin-5-yl)methyl)-5-iodo-1H-1,2,3-triazol-4-yl)methyl)-4-methoxybenzenesulfonamide
thiamim diphosphate analogue, EC50 value against Synechocystis sp. PCC 6803 is 0.0027 mM
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N-((1-((4-amino-2-methylpyrimidin-5-yl)methyl)-5-iodo-1H-1,2,3-triazol-4-yl)methyl)-4-methylbenzenesulfonamide
thiamim diphosphate analogue, EC50 value against Synechocystis sp. PCC 6803 is 0.002 mM
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N-((1-((4-amino-2-methylpyrimidin-5-yl)methyl)-5-iodo-1H-1,2,3-triazol-4-yl)methyl)-4-nitrobenzenesulfonamide
thiamim diphosphate analogue, EC50 value against Synechocystis sp. PCC 6803 is 0.0016 mM, EC50 value against Microcystis aeruginosa FACHB905 is 0.0001 mM
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N-ethylmaleimide
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1.1 mM, 50% inhibition
NaBH4
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rapid inactivation in the presence of thiamine diphosphate, may reduce thiamine diphosphate to produce a reversible inhibitor
NaCl
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at 2 M, 50% residual activity of enzyme expressed in Escherichia coli
O,O-dimethyl (2,3-dichlorophenoxyacetoxy)(furan-2-yl)-methylphosphonate
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O,O-dimethyl (2,3-dichlorophenoxyacetoxy)(thien-2-yl)-methylphosphonate
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O,O-dimethyl (2,4-dichlorophenoxyacetoxy)(furan-2-yl)-methylphosphonate
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O,O-dimethyl (2,4-dichlorophenoxyacetoxy)(thien-2-yl)-methylphosphonate
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O,O-dimethyl (2,6-dichlorophenoxyacetoxy)(furan-2-yl)-methylphosphonate
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O,O-dimethyl (2,6-dichlorophenoxyacetoxy)(thien-2-yl)-methylphosphonate
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O,O-dimethyl (2-chloro-5-methylphenoxyacetoxy)(furan-2-yl)methylphosphonate
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O,O-dimethyl (2-chloro-5-methylphenoxyacetoxy)(thien-2-yl)methylphosphonate
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O,O-dimethyl (3-fluorophenoxyacetoxy)(furan-2-yl)methylphosphonate
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O,O-dimethyl (3-fluorophenoxyacetoxy)(thien-2-yl)methylphosphonate
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O,O-dimethyl (4-chloro-2-methylphenoxyacetoxy)(furan-2-yl)methylphosphonate
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O,O-dimethyl (4-chloro-2-methylphenoxyacetoxy)(thien-2-yl)methylphosphonate
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O,O-dimethyl (4-chloro-3-methylphenoxyacetoxy)(furan-2-yl)methylphosphonate
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O,O-dimethyl (4-chloro-3-methylphenoxyacetoxy)(thien-2-yl)methylphosphonate
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O,O-dimethyl (4-chlorophenoxyacetoxy)(furan-2-yl)methylphosphonate
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O,O-dimethyl (4-chlorophenoxyacetoxy)(thien-2-yl)methylphosphonate
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O,O-dimethyl (4-fluorophenoxyacetoxy)(furan-2-yl)methylphosphonate
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p-chloromercuribenzenesulfonate
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8 mol per mol enzyme, complete inhibition
p-chloromercuribenzoate
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8 mol per mol enzyme, complete inhibition
pyruvate dehydrogenase kinase
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phosphorylation of E1p by pyruvate dehydrogenase kinase isoforms inactivates the pyruvate dehydrogenase complex
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sodium methyl [[[(2,4-dichlorophenoxy)acetyl]oxy](2,4-dichlorophenyl)methyl]phosphonate
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sodium methyl [[[(2,4-dichlorophenoxy)acetyl]oxy](3-nitrophenyl)methyl]phosphonate
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sodium methyl [[[(2,4-dichlorophenoxy)acetyl]oxy](4-fluorophenyl)methyl]phosphonate
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sodium methyl [[[(2,4-dichlorophenoxy)acetyl]oxy](4-methoxyphenyl)methyl]phosphonate
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sodium methyl [[[(2,4-dichlorophenoxy)acetyl]oxy](phenyl)methyl]phosphonate
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sodium o-methyl (2,4-dichlorophenoxyacetoxy)(2-chlorophenyl)methylphosphonate
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sodium o-methyl (2,4-dichlorophenoxyacetoxy)(3,4-dichlorophenyl)methyl phosphonate
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sodium o-methyl (2,4-dichlorophenoxyacetoxy)(4-chlorophenyl)methylphosphonate
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sodium o-methyl (2,4-dichlorophenoxyacetoxy)(4-methylphenyl)methylphosphonate
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sodium o-methyl (2,4-dichlorophenoxyacetoxy)(furan-2-yl)methylphosphonate
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sodium o-methyl (2,4-dichlorophenoxyacetoxy)(pyridin-2-yl)methylphosphonate
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Tetrahydrothiamine diphosphate
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cis-isomer, 0.0013 mM, 50% inhibition
thiamine 2-thiazolone diphosphate
crystallization data of complex with enzyme
thiamine 2-thiothiazolone diphosphate
thiamine thiazolone diphosphate
thiamine thiothiazolone diphosphate
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3-deazathiamine diphosphate
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competitive inhibitor, compound added to the culture medium for HeLa cells does not hamper the rate of cell growth and shows not significant impact on the viability of the cells
3-deazathiamine diphosphate
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competitive inhibitor
5-((4-((4-chlorophenoxy)methyl)-5-iodo-1H-1,2,3-triazol-1-yl)methyl)-2-methylpyrimidin-4-amine
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exhibits activity against Rhizoctonia solani even at 12.5 lg/ml and almost 5.5 times more inhibitory potency against Botryttis cinerea than pyrimethanil
5-((4-((4-chlorophenoxy)methyl)-5-iodo-1H-1,2,3-triazol-1-yl)methyl)-2-methylpyrimidin-4-amine
formation of intermolecular hydrogen bonding and halogen bonding. The 5-iodo-1,2,3-triazole and benzene ring play important roles in the biological activities of the compound. The iodine atom may participate in the halogen bonding with the negatively charged and can form a halogen bonding with the O atom of Asp521 in the active site of PDH-E1
Oxythiamine diphosphate
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competitive inhibitor, shows a significant cytostatic effect on HeLa cell culture
Oxythiamine diphosphate
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competitive inhibitor
phosphorylation
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phosphorylation
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phosphorylation inactivates recombinant alpha2,beta2 tetramer in about 10 min
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thiamine 2-thiothiazolone diphosphate
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thiamine 2-thiothiazolone diphosphate
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thiamine thiazolone diphosphate
inhibits potently the E1 component of the pyruvate dehydrogenase multienzyme complex PDHc, competitive to cofactor thiamine diphosphate, binding structure and determinants, binding induced reorganisation of the active site conformation, mechanism, K392 is important, overview
thiamine thiazolone diphosphate
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additional information
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effects of several plant hormones and auxin derivatives
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additional information
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enzyme from chloroplast is not inhibited by ATP
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additional information
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there is no significant change in the PDH activity in the presence of D-mannitol (35 mM)
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additional information
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not inhibited by ATP
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