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(1S,2S)-3-(2-hydroxy-4-methoxyphenyl)-1-(4-methoxyphenyl)propane-1,2-diol
-
AC50 value of 0.15 mM
(2R)-1-[(2,6-difluorophenyl)sulfonyl]-4-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-2-methylpiperazine
-
-
(2R)-4-[(2,6-difluorophenyl)sulfonyl]-1-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-2-methylpiperazine
-
-
(2R,3S)-2-phenyl-3,4-dihydro-2H-chromen-3-ol
-
AC50 value of 0.221 mM
(2R,3S)-5,7-diphenoxy-2-(3,4,5-triphenoxyphenyl)-3,4-dihydro-2H-1-benzopyran-3-ol
-
AC50 value of 0.028 mM
(2S)-1-[(2,6-difluorophenyl)sulfonyl]-4-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-2-methylpiperazine
-
-
(2S)-4-[(2,6-difluorophenyl)sulfonyl]-1-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-2-methylpiperazine
-
-
(3S)-7-phenoxy-2-(4-phenoxyphenyl)-3,4-dihydro-2H-1-benzopyran-3-ol
-
AC50 value of 0.115 mM
(3S,4S)-2-(3,4-diphenoxyphenyl)-5,7-diphenoxy-3,4-dihydro-2H-1-benzopyran-3,4-diol
-
AC50 value of 0.048 mM
1-acetyl-N-(3,4-dimethylphenyl)-1,2,3,4-tetrahydroquinoline-8-sulfonamide
-
-
1-acetyl-N-(3,4-dimethylphenyl)-2,3-dihydro-1H-indole-5-sulfonamide
-
-
1-[(2,6-difluorophenyl)sulfonyl]-4-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)piperazin-2-one
-
-
1-[1-(ethylsulfonyl)-2,3-dihydro-1H-indol-5-yl]-2-[(4-methoxyphenyl)sulfanyl]ethanone
-
-
2,3-dihydro-1,4-benzodioxin-6-yl[2-methyl-1-(methylsulfonyl)-2,3-dihydro-1H-indol-5-yl]methanone
-
-
2,6-difluorophenyl 5-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-2-methyl-2,3-dihydro-1H-indole-1-sulfonate
-
-
2-((2,3-dihydrobenzo[b][1,4]dioxin-6-yl)thio)-1-(2-methyl-1-(methylsulfonyl)indolin-5-yl) ethanone
-
-
2-(2,3-dihydro-1,4-benzodioxin-6-ylsulfanyl)-1-[2-methyl-1-(methylsulfonyl)-2,3-dihydro-1H-indol-5-yl]ethanone
-
-
2-(3,4-dihydro-2H-1,5-benzodioxepin-7-ylsulfanyl)-1-[1-(ethylsulfonyl)-2,3-dihydro-1H-indol-5-yl]ethanone
-
-
2-oxo-N-(pyridin-3-yl)-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
-
2-oxo-N-(pyridin-4-yl)-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
-
2-oxo-N-(quinolin-6-yl)-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
-
2-oxo-N-[3-(trifluoromethyl)phenyl]-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
-
2-[(3,5-difluorophenyl)sulfanyl]-1-[1-(ethylsulfonyl)-2,3-dihydro-1H-indol-5-yl]ethanone
-
-
3-(2-hydroxy-4-phenoxyphenyl)-1-(4-phenoxyphenyl)propane-1,2-diol
-
AC50 value of 0.2 mM
3-([4-[(2,6-difluoro-4-methoxyphenyl)sulfonyl]-1,4-diazepan-1-yl]sulfonyl)aniline
-
-
3-([4-[(2,6-difluoro-4-methoxyphenyl)sulfonyl]piperazin-1-yl]sulfonyl)aniline
-
highly potent activator of PKM2
3-([4-[(2,6-difluorophenyl)sulfonyl]piperazin-1-yl]sulfonyl)aniline
-
highly potent activator of PKM2
3-chloro-N-(3,4-dimethylphenyl)benzenesulfonamide
-
-
3-fluorophenyl (3,4-dimethylphenyl)sulfamate
-
-
3-fluorophenyl 5-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-2,3-dihydro-1H-indene-1-sulfonate
-
-
3-methoxyphenyl 5-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-2-methyl-2,3-dihydro-1H-indole-1-sulfonate
-
-
3-[(3,4-dimethylphenyl)sulfamoyl]benzoic acid
-
-
3-[[4-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-1,4-diazepan-1-yl]sulfonyl]aniline
-
highly potent activator of PKM2
3-[[4-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)piperazin-1-yl]sulfonyl]aniline
-
highly potent activator of PKM2
3-{[4-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-1,4-diazepan-1-yl]sulfonyl}aniline
-
i.e. NCGC00185916
4-fluorophenyl (3,4-dimethylphenyl)sulfamate
-
-
4-fluorophenyl 5-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-2-methyl-2,3-dihydro-1H-indole-1-sulfonate
-
-
4-[(2,6-difluorophenyl)sulfonyl]-1-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)piperazin-2-one
-
-
5-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-1-(methylsulfonyl)-1H-indole
-
-
5-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-2-methyl-1-(methylsulfonyl)-2,3-dihydro-1H-indole
-
-
5-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-2-methyl-1-(phenylsulfonyl)-2,3-dihydro-1H-indole
-
-
5-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-3-methyl-1-(methylsulfonyl)-1H-indole
-
-
5-amino-N-(3,4-dimethylphenyl)-1-methyl-1H-indole-7-sulfonamide
-
-
5-methoxy-2-[(2E)-3-(4-methoxyphenyl)prop-2-en-1-yl]phenol
-
AC50 value of 0.027 mM
6-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-1-(methylsulfonyl)-1,2,3,4-tetrahydroquinoline
-
-
6-(3-methoxybenzyl)-4-methyl-2-(methylsulfinyl)-4,6-dihydro-5H-thieno[2',3':4,5]pyrrolo[2,3-d]pyridazin-5-one
-
i.e. NCGC00186527
6-([4-[(2,6-difluorophenyl)sulfonyl]cyclohexyl]sulfonyl)-2,3-dihydro-1,4-benzodioxine
-
-
6-chloro-N-(3,4-dimethylphenyl)-3-oxo-3,4-dihydro-2H-1,4-benzoxazine-7-sulfonamide
-
-
6-{hydroxy[1-(methylsulfonyl)-1,2,3,7a-tetrahydro-5H-inden-5-ylidene]oxido-l6-sulfanyl}-2,3-dihydro-1,4-benzodioxine
-
-
6-{[1-(cyclopropylsulfonyl)-2,3-dihydro-1H-inden-5-yl]sulfonyl}-2,3-dihydro-1,4-benzodioxine
-
-
6-{[1-(ethylsulfonyl)-2,3-dihydro-1H-inden-5-yl]sulfonyl}-2,3-dihydro-1,4-benzodioxine
-
-
6-{[1-(methylsulfonyl)-2,3-dihydro-1H-inden-5-yl]sulfonyl}-2,3-dihydro-1,4-benzodioxine
-
-
6-{[1-(phenylsulfonyl)-2,3-dihydro-1H-inden-5-yl]sulfonyl}-2,3-dihydro-1,4-benzodioxine
-
-
6-{[2-(ethylsulfonyl)-2,3-dihydro-1H-inden-5-yl]sulfonyl}-2,3-dihydro-1,4-benzodioxine
-
-
6-{[2-(methylsulfonyl)-2,3-dihydro-1H-inden-5-yl]sulfonyl}-2,3-dihydro-1,4-benzodioxine
-
-
6-{[2-(phenylsulfonyl)-2,3-dihydro-1H-inden-5-yl]sulfonyl}-2,3-dihydro-1,4-benzodioxine
-
-
6-{[2-(tert-butylsulfonyl)-2,3-dihydro-1H-inden-5-yl]sulfonyl}-2,3-dihydro-1,4-benzodioxine
-
-
7-(chloroamino)-N-(3,4-dimethylphenyl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
-
7-(diethylamino)-N-(3,4-dimethylphenyl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
-
7-(dimethylamino)-N-(3,4-dimethylphenyl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
-
7-(fluoroamino)-N-(3-fluoro-4-methylphenyl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
-
7-bromo-N-(3,4-dimethylphenyl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
-
7-bromo-N-(4-chloro-3-methylphenyl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
-
7-chloro-N-(4-chloro-3-methylphenyl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
-
7-[3-(dimethylamino)pyrrolidin-1-yl]-N-(3,4-dimethylphenyl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
-
ATP
slight activation of the full-length enzyme, not the C-terminally truncated enzyme
CO2
-
activation, kinetics
cysteine
-
activation, can replace dithiothreitol
D-fructose 1,6-bisphosphate
D-fructose 1,6-diphosphate
D-fructose 2,6-bisphosphate
D-fructose 2,6-diphosphate
D-fructose 6-phosphate
-
requirement with Mg2+, activation with Mn2+
D-fructose-1,6-bisphosphate
D-glucose 1,6-diphosphate
-
slight activation
D-ribose 1-diphosphate 5-phosphate
-
activation, kinetics, much more effective than fructose 1,6-diphosphate or glucose 1,6-diphosphate
D-Ribulose 1,5-diphosphate
D-tagatose 1,6-diphosphate
-
requirement with Mg2+, activation with Mn2+
D-tagatose 6-phosphate
-
requirement with Mg2+, activation with Mn2+
dihydroxyacetone phosphate
erythrose 4-phosphate
-
requirement with Mg2+, activation with Mn2+
fructose 1,6-bisphosphate
fructose 2,6-bisphosphate
fructose-1,6-bisphosphate
glutamic acid
-
activation
glyceraldehyde 3-phosphate
GSH
-
activation, can replace dithiothreittol
isoleucine
-
slight activation, kinetics
isopropyl-beta-D-thiogalactopyranoside
-
50% increased activity at 1 mM
methyl paraoxon
-
in larvae, low doses of methyl paraoxon and methyl parathion activatd the enzyme but as the dose increases the Km value returned to normal levels
methyl parathion
-
in larvae, low doses of methyl paraoxon and methyl parathion activated the enzyme but as the dose increases the Km value returned to normal levels
Monovalent anions
-
activation, in decreasing order of efficiency: Cl-, Br-, NO3-
-
N-(2,3-dihydro-1,4-benzodioxin-6-yl)-2-methyl-1-(methylsulfonyl)-2,3-dihydro-1H-indole-5-sulfonamide
-
-
N-(2,3-dihydro-1,4-benzodioxin-6-yl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
-
N-(2,3-dihydro-1H-inden-5-yl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
-
N-(2-fluorophenyl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
-
N-(2-methylphenyl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
-
N-(3,4-dichlorophenyl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
-
N-(3,4-dimethylphenyl)-1-methyl-2-oxo-2,3-dihydro-1H-indole-5-sulfonamide
-
-
N-(3,4-dimethylphenyl)-2,2-dimethyl-3,4-dihydro-2H-chromene-6-sulfonamide
-
-
N-(3,4-dimethylphenyl)-2-oxo-1,2,3,4-tetrahydroquinoline-7-sulfonamide
-
i.e. NCGC00185939
N-(3,4-dimethylphenyl)-2-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine-7-sulfonamide
-
-
N-(3,4-dimethylphenyl)-2-oxo-2,3-dihydro-1H-benzimidazole-4-sulfonamide
-
-
N-(3,4-dimethylphenyl)-2-oxo-2,3-dihydro-1H-indole-4-sulfonamide
-
-
N-(3,4-dimethylphenyl)-2-oxo-7-(piperidin-1-yl)-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
-
N-(3,4-dimethylphenyl)-2-oxo-7-(propan-2-ylamino)-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
-
N-(3,4-dimethylphenyl)-2-oxo-7-(pyrrolidin-1-yl)-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
-
N-(3,4-dimethylphenyl)-3-methyl-2-oxo-2,3-dihydro-1,3-benzoxazole-5-sulfonamide
-
-
N-(3,4-dimethylphenyl)-3-oxo-3,4-dihydro-2H-1,4-benzoxazine-6-sulfonamide
-
-
N-(3,4-dimethylphenyl)-3-oxo-6-phenyl-3,4-dihydro-2H-1,4-benzoxazine-7-sulfonamide
-
-
N-(3,4-dimethylphenyl)-3-oxo-6-[(E)-2-phenylethenyl]-3,4-dihydro-2H-1,4-benzoxazine-7-sulfonamide
-
-
N-(3,4-dimethylphenyl)-4-(2-oxopyrrolidin-1-yl)benzenesulfonamide
-
-
N-(3,4-dimethylphenyl)-4-fluorobenzenesulfonamide
-
-
N-(3,4-dimethylphenyl)-4-methoxybenzenesulfonamide
-
-
N-(3,4-dimethylphenyl)-4-methyl-3,4-dihydro-2H-1,4-benzoxazine-6-sulfonamide
-
-
N-(3,4-dimethylphenyl)-6-fluoro-3-oxo-3,4-dihydro-2H-1,4-benzoxazine-7-sulfonamide
-
-
N-(3,4-dimethylphenyl)-6-methyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazine-7-sulfonamide
-
-
N-(3,4-dimethylphenyl)-7-(methylamino)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
-
N-(3,4-dimethylphenyl)-7-[(1-hydroxypropan-2-yl)amino]-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
-
N-(3,4-dimethylphenyl)-7-[(2-hydroxyethyl)amino]-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
-
N-(3,4-dimethylphenyl)-7-[(2-hydroxypropan-2-yl)amino]-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
-
N-(3,4-dimethylphenyl)-7-{[(2R)-1-hydroxypropan-2-yl]amino}-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
-
N-(3,4-dimethylphenyl)-7-{[(2S)-1-hydroxypropan-2-yl]amino}-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
-
N-(3,4-dimethylphenyl)naphthalene-2-sulfonamide
-
-
N-(3-chloro-4-fluorophenyl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
-
N-(3-chloro-4-methylphenyl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
-
N-(3-chloro-4-methylphenyl)-7-(fluoroamino)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
-
N-(3-chlorophenyl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
-
N-(3-fluoro-4-methylphenyl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
-
N-(3-fluoro-4-methylphenyl)-7-{[(2S)-1-hydroxypropan-2-yl]amino}-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
-
N-(3-methoxyphenyl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
-
N-(3-methylphenyl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
-
N-(4-chloro-3-fluorophenyl)-7-(fluoroamino)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
-
N-(4-chloro-3-fluorophenyl)-7-{[(2S)-1-hydroxypropan-2-yl]amino}-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
-
N-(4-chloro-3-methylphenyl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
-
N-(4-chloro-3-methylphenyl)-7-(fluoroamino)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
-
N-(4-chloro-3-methylphenyl)-7-{[(2S)-1-hydroxypropan-2-yl]amino}-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
-
N-(4-chlorophenyl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
-
N-(4-fluoro-3-methylphenyl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
-
N-(4-methoxyphenyl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
-
N-(4-methylphenyl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
-
N-(biphenyl-3-yl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
-
N-(naphthalen-2-yl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
-
N-[1-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)piperidin-4-yl]-2,6-difluorobenzenesulfonamide
-
-
N-[1-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)pyrrolidin-3-yl]-2,6-difluorobenzenesulfonamide
-
-
N-[1-[(2,6-difluorophenyl)sulfonyl]azetidin-3-yl]-2,3-dihydro-1,4-benzodioxine-6-sulfonamide
-
-
N-[1-[(2,6-difluorophenyl)sulfonyl]piperidin-4-yl]-2,3-dihydro-1,4-benzodioxine-6-sulfonamide
-
-
N-[1-[(2,6-difluorophenyl)sulfonyl]pyrrolidin-3-yl]-2,3-dihydro-1,4-benzodioxine-6-sulfonamide
-
-
N-[2-methyl-1-(methylsulfonyl)-2,3-dihydro-1H-indol-5-yl]-2,3-dihydro-1,4-benzodioxine-6-sulfonamide
-
-
N-[4-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-3-methylphenyl]-N-ethylmethanesulfonamide
-
-
N-[4-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)phenyl]-N-(propan-2-yl)methanesulfonamide
-
-
N-[4-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)phenyl]-N-ethylmethanesulfonamide
-
-
N-[[1-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)azetidin-3-yl]methyl]-2,6-difluorobenzenesulfonamide
-
-
N-{3-[(3,4-dimethylphenyl)sulfamoyl]phenyl}acetamide
-
-
N-{4-[(2,3-dihydro-1,4-benzodioxin-6-ylsulfanyl)acetyl]phenyl}methanesulfonamide
-
-
N-{4-[(3,4-dimethylphenyl)sulfamoyl]phenyl}acetamide
-
-
phenyl 5-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-2-methyl-2,3-dihydro-1H-indole-1-sulfonate
-
-
ribulose 5-phosphate
-
activation
succinyl-5-aminoimidazole-4-carboxamide-1-ribose 5'-phosphate
SAICAR, an endogenous metabolite that correlates with an increased level of cell proliferation, it activates pyruvate kinase isoform M2 (PKM2) in its dimeric form, connection between SAICAR binding and the oligomeric state of PKM2, SAICAR stimulates the PKM2 dimer without inducing formation of a PKM2 tetramer. SAICAR binds to PKM2 mutant G415R better than it binds to wild-type PKM2
-
Triton X-100
-
50% increase of activity of the bound enzyme only
3-phosphoglycerate
-
slight activation
3-phosphoglycerate
allosteric activator. Regulation of the enzyme by a carboxylate molecule rather than a sugar phosphate may reflect a step in the evolution of glycolysis that predates the dominance of sugars in metabolism
6-phosphogluconate
-
192% of activity at 0.05 mM
6-phosphogluconate
-
at 1 mM, 200% of activity
alanine
-
activation
AMP
9% activation at 0.1 mM, cPK3
AMP
wild-type, A0.5 value 0.013 mM
AMP
-
allosteric activator
asparagine
Busycotypus canaliculatum
-
activation
asparagine
-
synergistic activation with fructose 1,6-diphosphate of isozyme PK-aerobic, not PK-anoxic
aspartate
-
allosteric activator
D-fructose 1,6-bisphosphate
-
heterotropic activator of PK1, the modulation of oligomeric state by the allosteric effector D-fructose 1,6-bisphosphate does not occur at a concentration of 10 nM or above
D-fructose 1,6-bisphosphate
-
-
D-fructose 1,6-bisphosphate
activates
D-fructose 1,6-bisphosphate
20.5% increase of activity at 2.5 mM
D-fructose 1,6-bisphosphate
-
the smallest allosteric response to D-fructose 1,6-bisphosphate occurs at pH 6.5 and increases up to pH 8.0
D-fructose 1,6-bisphosphate
-
induces an association of two inactive dimers to the active tetrameric form
D-fructose 1,6-bisphosphate
triggers allosteric signal transduction, increases activity, binding tetramerizes the enzyme, whereas its release causes dissociation to inactive dimer
D-fructose 1,6-bisphosphate
-
-
D-fructose 1,6-bisphosphate
-
induces an association of two inactive dimers to the active tetrameric form. M2-PK showing ProTalpha kinase activity is a trimeric association and possesses no observable pyruvate kinase activity. This association can be shifted by fructose 1,6-P2 to the tetrameric form which results in a reduction of ProTalpha-kinase activity
D-fructose 1,6-bisphosphate
-
-
D-fructose 1,6-bisphosphate
-
strong activation
D-fructose 1,6-bisphosphate
increases the affinity and reduces the cooperativity of substrate binding, increases Vmax by 20%
D-fructose 1,6-diphosphate
-
activation
D-fructose 1,6-diphosphate
-
activation
D-fructose 1,6-diphosphate
-
pH-dependent
D-fructose 1,6-diphosphate
-
activation
D-fructose 1,6-diphosphate
-
not
D-fructose 1,6-diphosphate
-
-
D-fructose 1,6-diphosphate
-
activation
D-fructose 1,6-diphosphate
-
kinetics
D-fructose 1,6-diphosphate
Busycotypus canaliculatum
-
activation
D-fructose 1,6-diphosphate
Busycotypus canaliculatum
-
stimulates aerobic isozyme more strongly than anoxic isozyme
D-fructose 1,6-diphosphate
Busycotypus canaliculatum
-
synergism with Asp, PK-aerobic, not PK-anoxic
D-fructose 1,6-diphosphate
-
activation
D-fructose 1,6-diphosphate
-
not
D-fructose 1,6-diphosphate
-
not
D-fructose 1,6-diphosphate
-
activation
D-fructose 1,6-diphosphate
-
not
D-fructose 1,6-diphosphate
-
activation
D-fructose 1,6-diphosphate
-
major allosteric activator
D-fructose 1,6-diphosphate
-
activation
D-fructose 1,6-diphosphate
-
requirement with Mg2+
D-fructose 1,6-diphosphate
-
with Mn2+
D-fructose 1,6-diphosphate
-
activation
D-fructose 1,6-diphosphate
-
only PK II, shifting sigmoidal kinetics to hyperbolic curves, decrease in Km
D-fructose 1,6-diphosphate
-
activation
D-fructose 1,6-diphosphate
-
activation
D-fructose 1,6-diphosphate
-
activation
D-fructose 1,6-diphosphate
-
activation
D-fructose 1,6-diphosphate
-
not
D-fructose 1,6-diphosphate
-
strong activation, fat body enzyme
D-fructose 1,6-diphosphate
-
activation
D-fructose 1,6-diphosphate
-
heterotropic allosteric activator
D-fructose 1,6-diphosphate
-
activation
D-fructose 1,6-diphosphate
-
not
D-fructose 1,6-diphosphate
-
activation
D-fructose 1,6-diphosphate
-
isoform Pyk1p: is activated up to 8fold with Km lowered up to 30fold, Pyk2p: activity and Km only marginally affected
D-fructose 1,6-diphosphate
-
activation
D-fructose 1,6-diphosphate
-
kinetics
D-fructose 1,6-diphosphate
-
D-fructose 1,6-diphosphate
-
activation
D-fructose 1,6-diphosphate
-
more evident in the presence of glycerol
D-fructose 1,6-diphosphate
-
D-fructose 1,6-diphosphate
-
not
D-fructose 1,6-diphosphate
-
not
D-fructose 1,6-diphosphate
-
activation
D-fructose 1,6-diphosphate
-
not
D-fructose 1,6-diphosphate
not
D-fructose 1,6-diphosphate
-
activation
D-fructose 1,6-diphosphate
-
slight
D-fructose 1,6-diphosphate
-
kinetics
D-fructose 1,6-diphosphate
-
allosteric activation together with phosphoenolpyruvate
D-fructose 1,6-diphosphate
-
not
D-fructose 2,6-bisphosphate
allosteric stimulation
D-fructose 2,6-bisphosphate
wild-type, S0.5 value 0.000082 mM
D-fructose 2,6-bisphosphate
-
D-fructose 2,6-diphosphate
Busycotypus canaliculatum
-
activation
D-fructose 2,6-diphosphate
-
allosteric effector
D-fructose 2,6-diphosphate
-
allosteric effector
D-fructose 2,6-diphosphate
-
not
D-fructose 2,6-diphosphate
-
activation
D-fructose 2,6-diphosphate
-
allosteric effector
D-fructose 2,6-diphosphate
-
activation
D-fructose 2,6-diphosphate
-
best activator
D-fructose diphosphate
-
activation
D-fructose diphosphate
-
activation
D-fructose diphosphate
-
activation
D-fructose diphosphate
-
enzyme form I
D-fructose diphosphate
-
activation
D-fructose diphosphate
-
cardiac and liver isozyme, together with phosphoenolpyruvate
D-fructose diphosphate
-
activation
D-fructose diphosphate
Pigeon
-
activation
D-fructose diphosphate
-
activation
D-fructose diphosphate
-
activation
D-fructose diphosphate
-
allosteric effector
D-fructose-1,6-bisphosphate
-
isozyme PKM2 requires D-fructose-1,6-bisphosphate to form the active tetramer, but isozyme PKM1 does not
D-fructose-1,6-bisphosphate
-
D-fructose-1,6-bisphosphate
-
allosteric effector, binds to PykF but not to PykA
D-glucose 1-phosphate
-
not
D-glucose 1-phosphate
-
slight activation, not isozyme PKp
D-glucose 6-phosphate
-
-
D-glucose 6-phosphate
-
isozyme PK II
D-glucose 6-phosphate
-
activation
D-glucose 6-phosphate
-
requirement with Mg2+, activation with Mn2+
D-glucose 6-phosphate
-
activation
D-glucose 6-phosphate
-
not: isozyme PKp
D-glucose 6-phosphate
-
activation
D-glucose 6-phosphate
-
requirement
D-glucose 6-phosphate
radically activates
D-glucose 6-phosphate
classic allosteric activation with a 6fold reduction in the apparent Km and no effect on the Vmax
D-glucose 6-phosphate
-
-
D-glucose 6-phosphate
-
not
D-ribose 5-phosphate
-
D-ribose 5-phosphate
-
activation
D-ribose 5-phosphate
-
isozyme PK II
D-ribose 5-phosphate
-
activation
D-ribose 5-phosphate
-
0.1 mM, allosteric activator
D-ribose 5-phosphate
wild-type, A0.5 value 0.0075 mM
D-ribose 5-phosphate
-
activation
D-ribose 5-phosphate
-
requirement with Mg2+, activation with Mn2+
D-ribose 5-phosphate
allosteric activator
D-ribose 5-phosphate
-
activation
D-Ribulose 1,5-diphosphate
-
activation
D-Ribulose 1,5-diphosphate
-
not
D-Ribulose 1,5-diphosphate
-
activation
D-Ribulose 1,5-diphosphate
-
kinetics
D-Ribulose 1,5-diphosphate
-
much more effective than fructose 1,6-diphosphate or glucose 1,6-diphosphate
dihydroxyacetone phosphate
-
activation
dihydroxyacetone phosphate
-
activation
dihydroxyacetone phosphate
-
requirement with Mg2+
dihydroxyacetone phosphate
-
with Mn2+
dihydroxyacetone phosphate
-
activation
dihydroxyacetone phosphate
-
kinetics
dithiothreitol
-
required for optimal activity
dithiothreitol
-
activation
fructose 1,6-bisphosphate
FBP, allosteric regulation, Pyk2 is dependent on FBP activation
fructose 1,6-bisphosphate
-
-
fructose 1,6-bisphosphate
-
fructose 1,6-bisphosphate
-
activates isozyme PKM2 by direct binding
fructose 1,6-bisphosphate
FBP, enzyme PKM2 is allosterically activated by the glycolytic metabolite
fructose 1,6-bisphosphate
FBP, FBP-mediated PKM2 activation requires the tetramerization of PKM2. The dimeric enzyme, e.g. mutant PKM2G415R, is in its tense form and cannot be activated by FBP
fructose 1,6-bisphosphate
FBP, molecular dynamics (MD) simulations of the human PKM2 (hPKM2) monomer in the absence (apo-hPKM2) or presence of FBP (hPKM2-FBP), the molecular dynamics simulations identify conformational changes in PKM2 associated with FBP binding, overview
fructose 1,6-bisphosphate
-
-
fructose 1,6-bisphosphate
-
-
fructose 1,6-bisphosphate
FBP, molecular dynamics simulations identify conformational changes in PKM2 associated with FBP binding
fructose 1,6-bisphosphate
-
mutant enzyme T298C shows no catalytic activity in the absence of the heterotrophic activator
fructose 1,6-bisphosphate
-
-
fructose 1,6-bisphosphate
-
-
fructose 1,6-bisphosphate
Ka of liver enzyme is 0.029 mM, of anoxic liver enzyme 0.0032 mM
fructose 1,6-bisphosphate
F16BP, lower activation
fructose 1,6-bisphosphate
F16BP, lower activation
fructose 1,6-bisphosphate
slight activation
fructose 1,6-bisphosphate
slight activation, the isozyme with Glu117 is an active K+-dependent enzyme, at the same substrate concentration, its Vmax in the absence of fructose 1,6-bisphosphate is 80% of that with its effector. VcIPK is activated 31fold by fructose 1,6-bisphosphate
fructose 2,6-bisphosphate
F26BP, a much more potent allosteric activator of trypanosomatid PYKs compared to fructose 1,6-bisphosphate, F16BP
fructose 2,6-bisphosphate
F26BP, a much more potent allosteric activator of trypanosomatid PYKs compared to fructose 1,6-bisphosphate, F16BP
fructose 2,6-bisphosphate
-
fructose 6-phosphate
slight activation
fructose 6-phosphate
moderate activation
fructose-1,6-bisphosphate
FBP, 22% activation at 1 mM, cPK1
fructose-1,6-bisphosphate
FBP, 4% activation at 1 mM, cPK2
fructose-1,6-bisphosphate
hLPYK is allosterically activated by fructose-1,6-bisphosphate (Fru-1,6-BP). The allosteric site, as defined by previous structural studies, is located in domain C between the phosphate-binding loop (residues 444-449) and the allosteric loop (residues 527-533). The 6'-phosphate of Fru-1,6-BP contributes to binding by interacting with the phosphate-binding loop (residues 444-449 between beta1 of sheet D and alpha22)
glucose 6-phosphate
G6P, an activator increasing the apparent maximal velocity of isozyme PYK-I, 1.5fold activation at 5 mM without affecting the affinity and cooperativity towards the PEP substrate. The binding of glucose 6-phosphate and oxalate, which potentially lock the enzyme in its active state, increase the thermal stability of the enzyme. PfPYK might be a V-type allosteric enzyme with respect to G6P. In silico docking of the activator G6P to the canonical effector site, the phosphate group of G6P forms a number of favorable interactions with the PO4-2 motif
glucose 6-phosphate
slight activation
glucose 6-phosphate
VcIIPK is activated 159fold by glucose 6-phosphate
glyceraldehyde 3-phosphate
-
activation
glyceraldehyde 3-phosphate
-
activation
glyceraldehyde 3-phosphate
-
requirement with Mg2+
glyceraldehyde 3-phosphate
-
with Mn2+
glyceraldehyde 3-phosphate
-
not
L-aspartate
-
Ka-value 0.31 mM, reverses inhibition by L-glutamate
L-serine
12% activation at 0.2 mM, cPK2
L-serine
-
allosteric activator of PKM2, activates isozyme PKM2 by direct binding
L-serine
-
an allosteric activator of PKM2, serine-dependent regulation of pyruvate kinase M2 and general control nonderepressible 2 kinase to modulate the flux of glycolytic intermediates in support of cell proliferation
phosphate
-
activation
phosphate
Pigeon
-
activation
phosphoenolpyruvate
-
homotropic activator of PK1, the modulation of oligomeric state by the allosteric effector phosphoenolpyruvate does not occur at a concentration of 10 nM or above
phosphorylated hexoses
-
activation
-
phosphorylated hexoses
-
activation
-
phosphorylated hexoses
-
requirement with Mg2+
-
phosphorylated hexoses
-
with Mn2+
-
phosphorylated hexoses
Pigeon
-
activation
-
ribose 5-phosphate
slight activation
ribose 5-phosphate
Rib 5-P, VcIIPK is activated 200fold by ribose 5-phosphate. the pyruvate kinase with Lys117 is a K+-independent enzyme displaying an allosteric activation by ribose 5-phosphate. In the K+-independent enzyme, Mn2+ may mimic the allosteric effect of ribose 5-phosphate
ribose 5-phosphate
the pyruvate kinase with Lys117 is a K+-independent enzyme displaying an allosteric activation by ribose 5-phosphate. In the K+-independent enzyme, Mn2+ may mimic the allosteric effect of ribose 5-phosphate
additional information
-
not activated by 6-phosphogluconate
-
additional information
no effect by L-serine and L-glutamate at 0.2 mM on cPK4, poor effect by fructose-1,6-bisphosphate at 1.0 mM
-
additional information
no effect by L-serine and L-glutamate at 0.2 mM on cPK4, poor effect by fructose-1,6-bisphosphate at 1.0 mM
-
additional information
no effect by L-serine and L-glutamate at 0.2 mM on cPK4, poor effect by fructose-1,6-bisphosphate at 1.0 mM
-
additional information
no effect by L-serine and L-glutamate at 0.2 mM on cPK4, poor effect by fructose-1,6-bisphosphate at 1.0 mM
-
additional information
no effect by L-serine and L-glutamate at 0.2 mM on cPK4, poor effect by fructose-1,6-bisphosphate at 1.0 mM
-
additional information
-
no effect by L-serine and L-glutamate at 0.2 mM on cPK4, poor effect by fructose-1,6-bisphosphate at 1.0 mM
-
additional information
no effect by L-serine and L-glutamate at 0.2 mM on cPK5
-
additional information
no effect by L-serine and L-glutamate at 0.2 mM on cPK5
-
additional information
no effect by L-serine and L-glutamate at 0.2 mM on cPK5
-
additional information
no effect by L-serine and L-glutamate at 0.2 mM on cPK5
-
additional information
no effect by L-serine and L-glutamate at 0.2 mM on cPK5
-
additional information
-
no effect by L-serine and L-glutamate at 0.2 mM on cPK5
-
additional information
poor effect by AMP at 0.1 mM on cPK1
-
additional information
poor effect by AMP at 0.1 mM on cPK1
-
additional information
poor effect by AMP at 0.1 mM on cPK1
-
additional information
poor effect by AMP at 0.1 mM on cPK1
-
additional information
poor effect by AMP at 0.1 mM on cPK1
-
additional information
-
poor effect by AMP at 0.1 mM on cPK1
-
additional information
poor effect by fructose-1,6-bisphosphate at 1 mM and L-glutamate at 0.2 mM on cPK3
-
additional information
poor effect by fructose-1,6-bisphosphate at 1 mM and L-glutamate at 0.2 mM on cPK3
-
additional information
poor effect by fructose-1,6-bisphosphate at 1 mM and L-glutamate at 0.2 mM on cPK3
-
additional information
poor effect by fructose-1,6-bisphosphate at 1 mM and L-glutamate at 0.2 mM on cPK3
-
additional information
poor effect by fructose-1,6-bisphosphate at 1 mM and L-glutamate at 0.2 mM on cPK3
-
additional information
-
poor effect by fructose-1,6-bisphosphate at 1 mM and L-glutamate at 0.2 mM on cPK3
-
additional information
-
the initial rate of catalysis is modulated by substrate activation by phosphoenolpyruvate and ADP, activation by AMP and inhibition by ATP, phosphate and carbamoyl phosphate
-
additional information
Busycotypus canaliculatum
-
interacting effects of various activators and inhibitors
-
additional information
glucose-6-phosphate (G6P) has no significant effect on the S0.5 and kcat of Pyk2
-
additional information
glucose-6-phosphate (G6P) has no significant effect on the S0.5 and kcat of Pyk2
-
additional information
-
glucose-6-phosphate (G6P) has no significant effect on the S0.5 and kcat of Pyk2
-
additional information
-
not activated by fructose 1,6-bisphosphate
-
additional information
-
1-(sulfonyl)-5-(arylsulfonyl)indoline as activators of the tumor cell specific M2 isoform of pyruvate kinase, synthesis, structure-activity relationship analysis, enzyme active site docking, enzymatic reaction kinetics, selectivity, and pharmaceutical properties, overview. Activating potencies of the compounds compared for isozymes PKM2 and PKM1
-
additional information
-
2-oxo-N-aryl-1,2,3,4-tetrahydroquinoline-6-sulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase, synthesis, structure-activity relationships, selectivity, and notable physiochemical properties are, overview
-
additional information
different modes of PKM2 activation by FBP and SAICAR, schematic overview
-
additional information
-
different modes of PKM2 activation by FBP and SAICAR, schematic overview
-
additional information
no stimulation: fructose 1,6-bisphosphate
-
additional information
-
no stimulation: fructose 1,6-bisphosphate
-
additional information
-
enzyme is not affected by fructose-1,6-bisphosphate and glucose 6-phosphate
-
additional information
no effects by fructose 1,6-bisphosphate or fructose 2,6-bisphosphate on the enzyme activity
-
additional information
-
no effects by fructose 1,6-bisphosphate or fructose 2,6-bisphosphate on the enzyme activity
-
additional information
no activation by fructose 1,6-bisphosphate
-
additional information
-
no activation by fructose 1,6-bisphosphate
-
additional information
-
no activation by glucose 1,6-diphosphate, 5'-IMP, 2',3'-AMP, 2',3'-GMP, 2',3'-UMP
-
additional information
-
not activated by fructose 1,6-bisphosphate
-
additional information
-
no allosteric or regulatory effects are observed in the presence of D-fructose 1,6-diphosphate, D-fructose 2,6-diphosphate, D-glucose 6-phosphate, D-ribose 5-phosphate, AMP, ATP, ITP, AMP, L-His, L-Ser, L-Ala, L-Glu, Gln, L-Thr, L-Met, Gly, L-le, L-Asn, L-Cys, L-Pro, L-Arg, L-Lys, L-Phe, L-Trp, L-Leu, L-Asp, L-Val (1 mM each), L-Tyr (0.5 mM), or 0.1 mM acetyl-CoA
-
additional information
no significant effect by D-fructose 6-phosphate and D-ribulose 1,5-bisphosphate
-
additional information
-
no significant effect by D-fructose 6-phosphate and D-ribulose 1,5-bisphosphate
-
additional information
L-aspartate has no significant effect on the activity of the liver enzyme at 0-20 mM
-
additional information
L-aspartate has no significant effect on the activity of the liver enzyme at 0-20 mM
-
additional information
-
L-aspartate has no significant effect on the activity of the liver enzyme at 0-20 mM
-
additional information
neither L-aspartate nor fructose 1,6-bisphosphate has an influence on muscle pyruvate kinase in terms of activation
-
additional information
neither L-aspartate nor fructose 1,6-bisphosphate has an influence on muscle pyruvate kinase in terms of activation
-
additional information
-
neither L-aspartate nor fructose 1,6-bisphosphate has an influence on muscle pyruvate kinase in terms of activation
-
additional information
-
citrate does not have any effect on PK activity at concentrations up to 10 mM. fructose 1,6-bisphoaphate also shows little propensity to effect PK activity under the conditions of this experiment up to a concentration of 10 mM
-
additional information
-
no activation by 6-phosphogluconate
-