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1,1'-[6-(1-phenyl-1H-pyrrol-2-yl)-1,3,5-triazine-2,4-diyl]bis(azepane)
1,1'-[6-[1-(3,5-dimethylphenyl)-1H-pyrrol-2-yl]-1,3,5-triazine-2,4-diyl]bis(azepane)
1,1,1,1-azodimethyl diamide
-
-
1-(2-phenylethyl)-1H-pyrrole
1-(3,5-dimethylphenyl)-1H-pyrrole
1-(3-phenylpropyl)-1H-pyrrole
1-[4-(1-benzyl-1H-tetrazol-5-yl)-4-[(prop-2-yn-1-yl)amino]piperidin-1-yl]-3-(3-methyl-3H-diazirin-3-yl)propan-1-one
1-[4-chloro-6-(1-phenyl-1H-pyrrol-2-yl)-1,3,5-triazin-2-yl]azepane
10-bromo-3-(butylsulfanyl)-6-(thiophen-2-yl)-6,7-dihydro[1,2,4]triazino[5,6-d][3,1]benzoxazepine
2,4,6-Trinitrobenzenesulfonic acid
2,4-bis(aziridin-1-yl)-6-(1-phenyl-1H-pyrrol-2-yl)-1,3,5-triazine
2,4-bis(aziridin-1-yl)-6-(1-phenylpyrrol-2-yl)-S-triazine
2,4-bis(morpholin-4-yl)-6-(1-phenyl-1H-pyrrol-2-yl)-1,3,5-triazine
2,4-bis[(oxiran-2-yl)methoxy]-6-(1-phenyl-1H-pyrrol-2-yl)-1,3,5-triazine
2,4-dichloro-6-(1-cyclohexyl-1H-pyrrol-2-yl)-1,3,5-triazine
2,4-dichloro-6-(1-phenyl-1H-pyrrol-2-yl)-1,3,5-triazine
2,4-dichloro-6-[1-(2-phenylethyl)-1H-pyrrol-2-yl]-1,3,5-triazine
2,4-dichloro-6-[1-(3,5-dimethylphenyl)-1H-pyrrol-2-yl]-1,3,5-triazine
2,4-dichloro-6-[1-(3-phenylpropyl)-1H-pyrrol-2-yl]-1,3,5-triazine
2-(1-benzyl-1H-pyrrol-2-yl)-4,6-dichloro-1,3,5-triazine
2-(1-phenyl-1H-pyrrol-2-yl)-4,6-di(piperidin-1-yl)-1,3,5-triazine
2-(1-phenyl-1H-pyrrol-2-yl)-4,6-di(pyrrolidin-1-yl)-1,3,5-triazine
2-chloro-4-(methanesulfonyl)benzoic acid
2-methyl-4-(3-phenyl[1,2,4]triazolo[3,4-b][1,3,4]thiadiazol-6-yl)quinoline
2-[(5-cyanopyridin-2-yl)(methyl)amino]ethyl 4-methyl-1,2,3-thiadiazole-5-carboxylate
2-[2-[2-(2-aminoethoxy)ethoxy]ethoxy]ethyl 2-(4-methoxyphenyl)-3-methyl-4-oxo-1,2,3,3a,4,9b-hexahydro[1]benzopyrano[3,4-b]pyrrole-1-carboxylate
3-(3-(3-(3-chlorophenyl)pyrrolidin-1-yl)-1,2,4-triazin-5-yl)aniline
-
3-(3-(3-(benzyloxy)phenyl)pyrrolidin-1-yl)-5-(5-methylfuran-2-yl)-1,2,4-triazine
-
3-(3-(3-chlorophenyl)pyrrolidin-1-yl)-5-(3,4-dimethoxyphenyl)-1,2,4-triazine
-
3-(3-(3-chlorophenyl)pyrrolidin-1-yl)-5-(3-nitrophenyl)-1,2,4-triazine
-
3-(3-(3-chlorophenyl)pyrrolidin-1-yl)-5-(5-(2-(trifluoromethyl)phenyl)furan-2-yl)-1,2,4-triazine
-
3-(3-(3-chlorophenyl)pyrrolidin-1-yl)-5-phenyl-1,2,4-triazine
-
3-(butylsulfanyl)-6-(5-methylfuran-2-yl)-6,7-dihydro[1,2,4]triazino[5,6-d][3,1]benzoxazepine
3-[3-(3-chlorophenyl)pyrrolidin-1-yl]-5-(5-methylfuran-2-yl)-1,2,4-triazine
-
4-(1-benzyl-1H-pyrrol-2-yl)-N,N-dibutyl-6-chloro-1,3,5-triazin-2-amine
4-(3-(3-(3-chlorophenyl)pyrrolidin-1-yl)-1,2,4-triazin-5-yl)aniline
-
4-(azepan-1-yl)-6-(1-benzyl-1H-pyrrol-2-yl)-N,N-dibutyl-1,3,5-triazin-2-amine
4-(azepan-1-yl)-N,N-dibutyl-6-(1-cyclohexyl-1H-pyrrol-2-yl)-1,3,5-triazin-2-amine
4-(azepan-1-yl)-N,N-dibutyl-6-(1-phenyl-1H-pyrrol-2-yl)-1,3,5-triazin-2-amine
4-(azepan-1-yl)-N,N-dibutyl-6-[1-(2-phenylethyl)-1H-pyrrol-2-yl]-1,3,5-triazin-2-amine
4-(azepan-1-yl)-N,N-dibutyl-6-[1-(3,5-dimethylphenyl)-1H-pyrrol-2-yl]-1,3,5-triazin-2-amine
4-(azepan-1-yl)-N,N-dibutyl-6-[1-(3-phenylpropyl)-1H-pyrrol-2-yl]-1,3,5-triazin-2-amine
4-(azepan-1-yl)-N,N-dihexyl-6-(1-phenyl-1H-pyrrol-2-yl)-1,3,5-triazin-2-amine
4-(azepan-1-yl)-N,N-dimethyl-6-(1-phenyl-1H-pyrrol-2-yl)-1,3,5-triazin-2-amine
4-chloro-N,N-dihexyl-6-(1-phenyl-1H-pyrrol-2-yl)-1,3,5-triazin-2-amine
5-(4-bromophenyl)-3-(3-(3-chlorophenyl)pyrrolidin-1-yl)-1,2,4-triazine
-
5-(5-methylfuran-2-yl)-3-(3-(3-(trifluoromethyl)phenyl)pyrrolidin-1-yl)-1,2,4-triazine
-
5-bromo-1,3-dimethylpyrimidine-2,4(1H,3H)-dione
6-(1-benzyl-1H-pyrrol-2-yl)-N2,N2-dibutyl-N4,N4-dihexyl-1,3,5-triazine-2,4-diamine
6-(1-phenyl-1H-pyrrol-2-yl)-1,3,5-triazine-2,4-diamine
7-Chloro-4-nitrobenzo-2-oxa-1,3-diazole
-
-
alpha,beta-methyleneadenosine triphosphate
cannot be hydrolyzed and blocks both NTPase and pyrophosphatase activities
aminomethylenediphosphonate
Ca2+-diphosphate
-
nonhydrolyzable substrate analogue
cAMP
-
58% inhibition at 0.1 mM
CDP
-
50% inhibition at 0.1 mM
D-glucose
-
non-competitive
D-Glucose-6-phosphate
-
competitive
Diazonium-1H-tetrazole
-
-
dipropan-2-yl [(E)-(2-benzoylhydrazinylidene)(hydroxyamino)methyl]phosphonate
free divalent cations
-
-
-
fructose-1,6-bisphosphate
-
-
GDP
-
19% inhibition at 0.1 mM
GMP
-
18% inhibition at 0.1 mM
GSH
activates up to 4 mM, and inhibits at higher concentrations
Guanidine nucleotides
-
-
-
hydroxymethylbisphosphonate
-
competitive with diphosphate
imidodiphosphoric acid
a nonhydrolyzable PPi analogue, inhibits by 50% at 2 mM
L-malate
-
allosteric mechanism
methyl 2-(4-methoxyphenyl)-3-methyl-4-oxo-3,4-dihydro[1]benzopyrano[3,4-b]pyrrole-1-carboxylate
methyl 3-amino-4-(propane-2-sulfonyl)thiophene-2-carboxylate
methyl 3-benzyl-2-(4-methoxyphenyl)-4-oxo-3,4-dihydro[1]benzopyrano[3,4-b]pyrrole-1-carboxylate
methylene diphosphate-Mg complex
-
competitive inhibition of MgPPi hydrolysis, binds at the active site
Methylenediphosphonate
-
competes with ATP and diphosphate for binding at the allosteric regulatory site involving Lys112
N'-(2,4,5-trichlorobenzene-1-sulfonyl)pyridine-3-carbohydrazide
N'-(2,6-dichlorophenyl)-5-nitrofuran-2-carbohydrazide
N,N-dibutyl-4-chloro-6-(1-cyclohexyl-1H-pyrrol-2-yl)-1,3,5-triazin-2-amine
N,N-dibutyl-4-chloro-6-(1-phenyl-1H-pyrrol-2-yl)-1,3,5-triazin-2-amine
N,N-dibutyl-4-chloro-6-[1-(2-phenylethyl)-1H-pyrrol-2-yl]-1,3,5-triazin-2-amine
N,N-dibutyl-4-chloro-6-[1-(3,5-dimethylphenyl)-1H-pyrrol-2-yl]-1,3,5-triazin-2-amine
N,N-dibutyl-4-chloro-6-[1-(3-phenylpropyl)-1H-pyrrol-2-yl]-1,3,5-triazin-2-amine
N-(2-[[(4-chlorophenyl)methyl]sulfanyl]ethyl)-3-methylbut-2-enamide
N-(3-chlorophenyl)-N'-(5-[[(4-chlorophenyl)sulfanyl]methyl]furan-2-yl)urea
N-[4-[(3,5-dichlorophenyl)sulfamoyl]phenyl]acetamide
N2,N2,N4,N4-tetramethyl-6-(1-phenyl-1H-pyrrol-2-yl)-1,3,5-triazine-2,4-diamine
N2,N4-dimethyl-6-(1-phenyl-1H-pyrrol-2-yl)-1,3,5-triazine-2,4-diamine
p-chloromercuribenzenesulfonic acid
-
-
p-chloromercuriphenyl sulfonate
-
50% inhibition of hydrolysis of diphosphate at 25 µM
phenylmercuric acetate
-
-
phenylmethanesulfonyl fluoride
-
-
Sodium fluoride
inhibition kinetics
UDP
-
35% inhibition at 0.1 mM
[1,1'-biphenyl]-2,2'-dicarbonitrile
1,1'-[6-(1-phenyl-1H-pyrrol-2-yl)-1,3,5-triazine-2,4-diyl]bis(azepane)
-
1,1'-[6-(1-phenyl-1H-pyrrol-2-yl)-1,3,5-triazine-2,4-diyl]bis(azepane)
-
1,1'-[6-[1-(3,5-dimethylphenyl)-1H-pyrrol-2-yl]-1,3,5-triazine-2,4-diyl]bis(azepane)
-
1,1'-[6-[1-(3,5-dimethylphenyl)-1H-pyrrol-2-yl]-1,3,5-triazine-2,4-diyl]bis(azepane)
-
1-(2-phenylethyl)-1H-pyrrole
-
1-(2-phenylethyl)-1H-pyrrole
-
1-(3,5-dimethylphenyl)-1H-pyrrole
-
1-(3,5-dimethylphenyl)-1H-pyrrole
-
1-(3-phenylpropyl)-1H-pyrrole
-
1-(3-phenylpropyl)-1H-pyrrole
-
1-benzyl-1H-pyrrole
-
1-cyclohexyl-1H-pyrrole
-
1-cyclohexyl-1H-pyrrole
-
1-[4-(1-benzyl-1H-tetrazol-5-yl)-4-[(prop-2-yn-1-yl)amino]piperidin-1-yl]-3-(3-methyl-3H-diazirin-3-yl)propan-1-one
-
1-[4-(1-benzyl-1H-tetrazol-5-yl)-4-[(prop-2-yn-1-yl)amino]piperidin-1-yl]-3-(3-methyl-3H-diazirin-3-yl)propan-1-one
-
1-[4-chloro-6-(1-phenyl-1H-pyrrol-2-yl)-1,3,5-triazin-2-yl]azepane
-
1-[4-chloro-6-(1-phenyl-1H-pyrrol-2-yl)-1,3,5-triazin-2-yl]azepane
-
10-bromo-3-(butylsulfanyl)-6-(thiophen-2-yl)-6,7-dihydro[1,2,4]triazino[5,6-d][3,1]benzoxazepine
-
10-bromo-3-(butylsulfanyl)-6-(thiophen-2-yl)-6,7-dihydro[1,2,4]triazino[5,6-d][3,1]benzoxazepine
-
2,4,6-Trinitrobenzenesulfonic acid
-
-
2,4,6-Trinitrobenzenesulfonic acid
-
-
2,4,6-Trinitrobenzenesulfonic acid
-
-
2,4-bis(aziridin-1-yl)-6-(1-phenyl-1H-pyrrol-2-yl)-1,3,5-triazine
-
2,4-bis(aziridin-1-yl)-6-(1-phenyl-1H-pyrrol-2-yl)-1,3,5-triazine
-
2,4-bis(aziridin-1-yl)-6-(1-phenylpyrrol-2-yl)-S-triazine
allosteric inhibitor
2,4-bis(aziridin-1-yl)-6-(1-phenylpyrrol-2-yl)-S-triazine
allosteric inhibitor
2,4-bis(morpholin-4-yl)-6-(1-phenyl-1H-pyrrol-2-yl)-1,3,5-triazine
-
2,4-bis(morpholin-4-yl)-6-(1-phenyl-1H-pyrrol-2-yl)-1,3,5-triazine
-
2,4-bis[(oxiran-2-yl)methoxy]-6-(1-phenyl-1H-pyrrol-2-yl)-1,3,5-triazine
-
2,4-bis[(oxiran-2-yl)methoxy]-6-(1-phenyl-1H-pyrrol-2-yl)-1,3,5-triazine
-
2,4-dichloro-6-(1-cyclohexyl-1H-pyrrol-2-yl)-1,3,5-triazine
-
2,4-dichloro-6-(1-cyclohexyl-1H-pyrrol-2-yl)-1,3,5-triazine
-
2,4-dichloro-6-(1-phenyl-1H-pyrrol-2-yl)-1,3,5-triazine
-
2,4-dichloro-6-(1-phenyl-1H-pyrrol-2-yl)-1,3,5-triazine
-
2,4-dichloro-6-[1-(2-phenylethyl)-1H-pyrrol-2-yl]-1,3,5-triazine
-
2,4-dichloro-6-[1-(2-phenylethyl)-1H-pyrrol-2-yl]-1,3,5-triazine
-
2,4-dichloro-6-[1-(3,5-dimethylphenyl)-1H-pyrrol-2-yl]-1,3,5-triazine
-
2,4-dichloro-6-[1-(3,5-dimethylphenyl)-1H-pyrrol-2-yl]-1,3,5-triazine
-
2,4-dichloro-6-[1-(3-phenylpropyl)-1H-pyrrol-2-yl]-1,3,5-triazine
-
2,4-dichloro-6-[1-(3-phenylpropyl)-1H-pyrrol-2-yl]-1,3,5-triazine
-
2-(1-benzyl-1H-pyrrol-2-yl)-4,6-dichloro-1,3,5-triazine
-
2-(1-benzyl-1H-pyrrol-2-yl)-4,6-dichloro-1,3,5-triazine
-
2-(1-phenyl-1H-pyrrol-2-yl)-4,6-di(piperidin-1-yl)-1,3,5-triazine
-
2-(1-phenyl-1H-pyrrol-2-yl)-4,6-di(piperidin-1-yl)-1,3,5-triazine
-
2-(1-phenyl-1H-pyrrol-2-yl)-4,6-di(pyrrolidin-1-yl)-1,3,5-triazine
-
2-(1-phenyl-1H-pyrrol-2-yl)-4,6-di(pyrrolidin-1-yl)-1,3,5-triazine
-
2-chloro-4-(methanesulfonyl)benzoic acid
-
2-chloro-4-(methanesulfonyl)benzoic acid
-
2-methyl-4-(3-phenyl[1,2,4]triazolo[3,4-b][1,3,4]thiadiazol-6-yl)quinoline
-
2-methyl-4-(3-phenyl[1,2,4]triazolo[3,4-b][1,3,4]thiadiazol-6-yl)quinoline
-
2-phosphoglyceric acid
-
in the absence of free Mg2+
2-phosphoglyceric acid
-
in the absence of free Mg2+
2-phosphoglyceric acid
-
in the absence of free Mg2+
2-[(5-cyanopyridin-2-yl)(methyl)amino]ethyl 4-methyl-1,2,3-thiadiazole-5-carboxylate
-
2-[(5-cyanopyridin-2-yl)(methyl)amino]ethyl 4-methyl-1,2,3-thiadiazole-5-carboxylate
-
2-[2-[2-(2-aminoethoxy)ethoxy]ethoxy]ethyl 2-(4-methoxyphenyl)-3-methyl-4-oxo-1,2,3,3a,4,9b-hexahydro[1]benzopyrano[3,4-b]pyrrole-1-carboxylate
-
2-[2-[2-(2-aminoethoxy)ethoxy]ethoxy]ethyl 2-(4-methoxyphenyl)-3-methyl-4-oxo-1,2,3,3a,4,9b-hexahydro[1]benzopyrano[3,4-b]pyrrole-1-carboxylate
-
3-(butylsulfanyl)-6-(5-methylfuran-2-yl)-6,7-dihydro[1,2,4]triazino[5,6-d][3,1]benzoxazepine
-
3-(butylsulfanyl)-6-(5-methylfuran-2-yl)-6,7-dihydro[1,2,4]triazino[5,6-d][3,1]benzoxazepine
-
4-(1-benzyl-1H-pyrrol-2-yl)-N,N-dibutyl-6-chloro-1,3,5-triazin-2-amine
-
4-(1-benzyl-1H-pyrrol-2-yl)-N,N-dibutyl-6-chloro-1,3,5-triazin-2-amine
-
4-(azepan-1-yl)-6-(1-benzyl-1H-pyrrol-2-yl)-N,N-dibutyl-1,3,5-triazin-2-amine
-
4-(azepan-1-yl)-6-(1-benzyl-1H-pyrrol-2-yl)-N,N-dibutyl-1,3,5-triazin-2-amine
-
4-(azepan-1-yl)-N,N-dibutyl-6-(1-cyclohexyl-1H-pyrrol-2-yl)-1,3,5-triazin-2-amine
-
4-(azepan-1-yl)-N,N-dibutyl-6-(1-cyclohexyl-1H-pyrrol-2-yl)-1,3,5-triazin-2-amine
-
4-(azepan-1-yl)-N,N-dibutyl-6-(1-phenyl-1H-pyrrol-2-yl)-1,3,5-triazin-2-amine
-
4-(azepan-1-yl)-N,N-dibutyl-6-(1-phenyl-1H-pyrrol-2-yl)-1,3,5-triazin-2-amine
-
4-(azepan-1-yl)-N,N-dibutyl-6-[1-(2-phenylethyl)-1H-pyrrol-2-yl]-1,3,5-triazin-2-amine
pecies-specific inhibitor
4-(azepan-1-yl)-N,N-dibutyl-6-[1-(2-phenylethyl)-1H-pyrrol-2-yl]-1,3,5-triazin-2-amine
pecies-specific inhibitor
4-(azepan-1-yl)-N,N-dibutyl-6-[1-(3,5-dimethylphenyl)-1H-pyrrol-2-yl]-1,3,5-triazin-2-amine
-
4-(azepan-1-yl)-N,N-dibutyl-6-[1-(3,5-dimethylphenyl)-1H-pyrrol-2-yl]-1,3,5-triazin-2-amine
-
4-(azepan-1-yl)-N,N-dibutyl-6-[1-(3-phenylpropyl)-1H-pyrrol-2-yl]-1,3,5-triazin-2-amine
-
4-(azepan-1-yl)-N,N-dibutyl-6-[1-(3-phenylpropyl)-1H-pyrrol-2-yl]-1,3,5-triazin-2-amine
-
4-(azepan-1-yl)-N,N-dihexyl-6-(1-phenyl-1H-pyrrol-2-yl)-1,3,5-triazin-2-amine
-
4-(azepan-1-yl)-N,N-dihexyl-6-(1-phenyl-1H-pyrrol-2-yl)-1,3,5-triazin-2-amine
-
4-(azepan-1-yl)-N,N-dimethyl-6-(1-phenyl-1H-pyrrol-2-yl)-1,3,5-triazin-2-amine
-
4-(azepan-1-yl)-N,N-dimethyl-6-(1-phenyl-1H-pyrrol-2-yl)-1,3,5-triazin-2-amine
-
4-chloro-N,N-dihexyl-6-(1-phenyl-1H-pyrrol-2-yl)-1,3,5-triazin-2-amine
-
4-chloro-N,N-dihexyl-6-(1-phenyl-1H-pyrrol-2-yl)-1,3,5-triazin-2-amine
-
4-hydroxymercuribenzoate
-
-
4-hydroxymercuribenzoate
-
-
4-hydroxymercuribenzoate
-
-
5-bromo-1,3-dimethylpyrimidine-2,4(1H,3H)-dione
-
5-bromo-1,3-dimethylpyrimidine-2,4(1H,3H)-dione
-
6-(1-benzyl-1H-pyrrol-2-yl)-N2,N2-dibutyl-N4,N4-dihexyl-1,3,5-triazine-2,4-diamine
-
6-(1-benzyl-1H-pyrrol-2-yl)-N2,N2-dibutyl-N4,N4-dihexyl-1,3,5-triazine-2,4-diamine
-
6-(1-phenyl-1H-pyrrol-2-yl)-1,3,5-triazine-2,4-diamine
-
6-(1-phenyl-1H-pyrrol-2-yl)-1,3,5-triazine-2,4-diamine
-
adenine nucleotide
a quarter of Family II PPases contain an autoinhibitory regulatory insert formed by two cystathionine beta-synthase (CBS) domains and one DRTGG domain. Adenine nucleotide binding either activates or inhibits the CBS domain-containing PPases, thereby tuning their activity and, hence, diphosphate levels, in response to changes in cell energy status (ATP/ADP ratio)
adenine nucleotide
a quarter of Family II PPases contain an autoinhibitory regulatory insert formed by two cystathionine beta-synthase (CBS) domains and one DRTGG domain. Adenine nucleotide binding either activates or inhibits the CBS domain-containing PPases, thereby tuning their activity and, hence, diphosphate levels, in response to changes in cell energy status (ATP/ADP ratio)
adenine nucleotide
a quarter of Family II PPases contain an autoinhibitory regulatory insert formed by two cystathionine beta-synthase (CBS) domains and one DRTGG domain. Adenine nucleotide binding either activates or inhibits the CBS domain-containing PPases, thereby tuning their activity and, hence, diphosphate levels, in response to changes in cell energy status (ATP/ADP ratio)
adenine nucleotide
a quarter of Family II PPases contain an autoinhibitory regulatory insert formed by two cystathionine beta-synthase (CBS) domains and one DRTGG domain. Adenine nucleotide binding either activates or inhibits the CBS domain-containing PPases, thereby tuning their activity and, hence, diphosphate levels, in response to changes in cell energy status (ATP/ADP ratio)
adenine nucleotide
a quarter of Family II PPases contain an autoinhibitory regulatory insert formed by two cystathionine beta-synthase (CBS) domains and one DRTGG domain. Adenine nucleotide binding either activates or inhibits the CBS domain-containing PPases, thereby tuning their activity and, hence, diphosphate levels, in response to changes in cell energy status (ATP/ADP ratio)
adenine nucleotide
a quarter of Family II PPases contain an autoinhibitory regulatory insert formed by two cystathionine beta-synthase (CBS) domains and one DRTGG domain. Adenine nucleotide binding either activates or inhibits the CBS domain-containing PPases, thereby tuning their activity and, hence, diphosphate levels, in response to changes in cell energy status (ATP/ADP ratio)
ADP
-
ADP
allosteric inhibition
ADP
-
partially inhibited
ADP
-
complete inhibition at 0.1 mM
aminomethylenediphosphonate
-
-
aminomethylenediphosphonate
-
-
AMP
the structures of the CBSPPase regulatory part contain AMP or diadenosine tetraphosphate (Ap4A) bound to the CBS domains in different modes. AMP is bound in each monomeric unit at the interface between its CBS domains, whereas one Ap4A molecule occupies both AMP-binding sites. The conformational states of the AMP- and Ap4A-bound CBS modules are significantly different, explaining the different effects of the nucleotides on enzyme activity
AMP
allosteric inhibition
AMP
the structures of the CBSPPase regulatory part contain AMP or diadenosine tetraphosphate (Ap4A) bound to the CBS domains in different modes. AMP is bound in each monomeric unit at the interface between its CBS domains, whereas one Ap4A molecule occupies both AMP-binding sites. The conformational states of the AMP- and Ap4A-bound CBS modules are significantly different, explaining the different effects of the nucleotides on enzyme activity
AMP
-
partially inhibited
AMP
-
96% inhibition at 0.1 mM
ATP
-
competes with methylenediphosphonate and diphosphate for binding at the allosteric regulatory site involving Lys112
ATP
50% inhibition at 2 mM, 90% at 3 mM ATP
ATP
-
partially inhibited
Ca2+
-
Ca2+
Aranda Christine
-
most effective inhibitor among the cations tested
Ca2+
-
activates at up to 1 mM, inhibits at higher concentrations, complete inhibition at 2 mM, overview
Ca2+
over 90% inhibition at 0.12 mM; over 90% inhibition at 0.12 mM
Ca2+
complete inhibition at 42 mM
Ca2+
enzymatic activity is inhibited more than 95% in the presence of 5 mM Ca2+
Ca2+
-
inhibits sPPase activity of the enzyme, 62% inhibition of p26.1a, 49% of p26.1b
Ca2+
-
less effective than Cd2+
Ca2+
-
50% at 0.012 mM: Mg2+ 0.4 mM
Ca2+
-
50% inhibition at 0.1 mM, no effect at physiological concentrations
Ca2+
inhibits the cleavage of diphosphate in the presence of 2.5 mM Mg2+. 0.01 mM CaCl2 inhibits the enzyme by about 50%
Cd2+
Aranda Christine
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-
Co2+
Aranda Christine
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-
Co2+
-
activates at up to 1 mM, inhibits at higher concentrations, overview
Co2+
can substitute for Mg2+ at concentrations up to 0.5 mM, inhibitory above
Co2+
-
less effective than Ca2+
Cu2+
-
Cu2+
-
less effective then Mn2+
diphosphate
high substrate inhibition at low levels of Mg2+
diphosphate
-
hydrolysis of imidophosphate competitively inhibited in the absence of divalent cations
diphosphate
-
competes with ATP and methylenediphosphonate for binding at the allosteric regulatory site involving Lys112
dipropan-2-yl [(E)-(2-benzoylhydrazinylidene)(hydroxyamino)methyl]phosphonate
-
dipropan-2-yl [(E)-(2-benzoylhydrazinylidene)(hydroxyamino)methyl]phosphonate
-
EDTA
-
EDTA
Aranda Christine
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EDTA
-
Na2SO4, Li2SO4 enhance deactivation, Mn2+ is protective
EDTA
-
89% activation at 0.9 mM, complete inhibition at 5 mM
EDTA
enzymatic activity is inhibited more than 70% in the presence of 5 mM EDTA
F-
Aranda Christine
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F-
-
Co2+ and Mn2+ protect against fluoride inhibition
fluoride
inhibition of wild-type and mutant enzyme
fluoride
inhibits Family I PPases at micromolar concentrations by replacing the nucleophilic water molecule. The effect of fluoride on Family II enzymes strongly depends on the metal cofactor in the tight binding site. Mn/Co enzymes are inhibited weakly by fluoride, but if the transition metal is replaced by Mg2+, fluoride binds 1000times tighter, achieving an affinity characteristic of Family I enzymes
fluoride
reversible inhibition, binds to the active site, binding structure, overview
fluoride
-
50% inhibition at 0.5 mM, 70-80% at 1.0 mM
fluoride
potent inhibition, IC50: 0.1 mM
fluoride
inhibits Family I PPases at micromolar concentrations by replacing the nucleophilic water molecule. The effect of fluoride on Family II enzymes strongly depends on the metal cofactor in the tight binding site. Mn/Co enzymes are inhibited weakly by fluoride, but if the transition metal is replaced by Mg2+, fluoride binds 1000times tighter, achieving an affinity characteristic of Family I enzymes
Guanidine HCl
-
-
Hg2+
-
Imidodiphosphate
-
-
iodoacetamide
-
-
iodoacetate
-
-
KF
-
90% at 0.5 mM
methyl 2-(4-methoxyphenyl)-3-methyl-4-oxo-3,4-dihydro[1]benzopyrano[3,4-b]pyrrole-1-carboxylate
-
methyl 2-(4-methoxyphenyl)-3-methyl-4-oxo-3,4-dihydro[1]benzopyrano[3,4-b]pyrrole-1-carboxylate
-
methyl 3-amino-4-(propane-2-sulfonyl)thiophene-2-carboxylate
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methyl 3-amino-4-(propane-2-sulfonyl)thiophene-2-carboxylate
-
methyl 3-benzyl-2-(4-methoxyphenyl)-4-oxo-3,4-dihydro[1]benzopyrano[3,4-b]pyrrole-1-carboxylate
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methyl 3-benzyl-2-(4-methoxyphenyl)-4-oxo-3,4-dihydro[1]benzopyrano[3,4-b]pyrrole-1-carboxylate
-
Mn2+
Aranda Christine
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-
Mn2+
-
activates at up to 1 mM, inhibits at higher concentrations, overview
Mn2+
-
60% inhibition at 1 mM Mn2+: 24 mM Mg2+
Mn2+
can substitute for Mg2+ at concentrations up to 0.5 mM, inhibitory above
Mn2+
-
less effective than Zn2+
N'-(2,4,5-trichlorobenzene-1-sulfonyl)pyridine-3-carbohydrazide
-
N'-(2,4,5-trichlorobenzene-1-sulfonyl)pyridine-3-carbohydrazide
-
N'-(2,6-dichlorophenyl)-5-nitrofuran-2-carbohydrazide
-
N'-(2,6-dichlorophenyl)-5-nitrofuran-2-carbohydrazide
-
N,N-dibutyl-4-chloro-6-(1-cyclohexyl-1H-pyrrol-2-yl)-1,3,5-triazin-2-amine
-
N,N-dibutyl-4-chloro-6-(1-cyclohexyl-1H-pyrrol-2-yl)-1,3,5-triazin-2-amine
-
N,N-dibutyl-4-chloro-6-(1-phenyl-1H-pyrrol-2-yl)-1,3,5-triazin-2-amine
-
N,N-dibutyl-4-chloro-6-(1-phenyl-1H-pyrrol-2-yl)-1,3,5-triazin-2-amine
-
N,N-dibutyl-4-chloro-6-[1-(2-phenylethyl)-1H-pyrrol-2-yl]-1,3,5-triazin-2-amine
-
N,N-dibutyl-4-chloro-6-[1-(2-phenylethyl)-1H-pyrrol-2-yl]-1,3,5-triazin-2-amine
-
N,N-dibutyl-4-chloro-6-[1-(3,5-dimethylphenyl)-1H-pyrrol-2-yl]-1,3,5-triazin-2-amine
-
N,N-dibutyl-4-chloro-6-[1-(3,5-dimethylphenyl)-1H-pyrrol-2-yl]-1,3,5-triazin-2-amine
-
N,N-dibutyl-4-chloro-6-[1-(3-phenylpropyl)-1H-pyrrol-2-yl]-1,3,5-triazin-2-amine
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N,N-dibutyl-4-chloro-6-[1-(3-phenylpropyl)-1H-pyrrol-2-yl]-1,3,5-triazin-2-amine
-
N-(2-[[(4-chlorophenyl)methyl]sulfanyl]ethyl)-3-methylbut-2-enamide
-
N-(2-[[(4-chlorophenyl)methyl]sulfanyl]ethyl)-3-methylbut-2-enamide
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N-(3-chlorophenyl)-N'-(5-[[(4-chlorophenyl)sulfanyl]methyl]furan-2-yl)urea
-
N-(3-chlorophenyl)-N'-(5-[[(4-chlorophenyl)sulfanyl]methyl]furan-2-yl)urea
-
N-ethylmaleimide
-
-
N-ethylmaleimide
inhibits 38% of PPase activity at 37.5 mM
N-[4-[(3,5-dichlorophenyl)sulfamoyl]phenyl]acetamide
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N-[4-[(3,5-dichlorophenyl)sulfamoyl]phenyl]acetamide
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N2,N2,N4,N4-tetramethyl-6-(1-phenyl-1H-pyrrol-2-yl)-1,3,5-triazine-2,4-diamine
-
N2,N2,N4,N4-tetramethyl-6-(1-phenyl-1H-pyrrol-2-yl)-1,3,5-triazine-2,4-diamine
-
N2,N4-dimethyl-6-(1-phenyl-1H-pyrrol-2-yl)-1,3,5-triazine-2,4-diamine
-
N2,N4-dimethyl-6-(1-phenyl-1H-pyrrol-2-yl)-1,3,5-triazine-2,4-diamine
-
NaF
-
-
NaF
inhibits 46% and 91.4% of the activity at 0.04 mM and 0.5 mM, respectively
p-chloromercuribenzoate
-
-
p-chloromercuribenzoate
-
-
p-chloromercuribenzoate
-
-
P2O74-
-
-
Phenylglyoxal
-
-
Phenylglyoxal
the inhibitory effect of phenylglyoxal is higher at 56°C than at room temperature. With 5 mM phenylglyoxal almost complete inhibition can be observed after 15 min incubation at 56°C
Phosphonates
-
-
SDS
-
-
SDS
SDS acts as a mixed-type reversible inhibitor of PPase, PPase can be fully inactivated at SDS concentration of 2 mM
Zn2+
-
-
Zn2+
-
activates at up to 1 mM, inhibits at higher concentrations, overview
Zn2+
-
inhibition caused at a separate site rather than as Zn-diphosphate substrate
Zn2+
can substitute for Mg2+ at concentrations up to 0.5 mM, inhibitory above
Zn2+
-
less effective then Co2+
[1,1'-biphenyl]-2,2'-dicarbonitrile
-
[1,1'-biphenyl]-2,2'-dicarbonitrile
-
additional information
C-substituted derivatives of methylene bisphosphonate, which are nonhydrolyzable diphosphate analogues, bind to Family II PPases 2-3 orders of magnitude more weakly than to Family I enzymes, whereas PNP binds with similar affinity, regardless of the metal cofactor bound. Structure-function analysis of canonical Family II PPases, catalytic reaction mechanism, detailed, overview
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additional information
inorganic diphosphatase containing a pair of regulatory CBS domains (CBS-PPase1) is allosterically inhibited by AMP and ADP and activated by ATP and diadenosine polyphosphates
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additional information
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inorganic diphosphatase containing a pair of regulatory CBS domains (CBS-PPase1) is allosterically inhibited by AMP and ADP and activated by ATP and diadenosine polyphosphates
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additional information
discovery and synthesis of analogues of lead compound allosteric inhibitor (2,4-bis(aziridin-1-yl)-6-(1-phenylpyrrol-2-yl)-S-triazine) as inhibitors of bacterial PPiases
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additional information
XM_008360526
apple S-RNase binds to two variable regions of MdPPa, resulting in a noncompetitive inhibition of its activity
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additional information
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apple S-RNase binds to two variable regions of MdPPa, resulting in a noncompetitive inhibition of its activity
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additional information
not inhibited by nucleotides or its end product phosphate: neither addition of 0.75 mM AMP or 0.005 mM ADP nor addition of up to 1.5 mM phosphate led to a reduced reaction rate
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additional information
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not inhibited by nucleotides or its end product phosphate: neither addition of 0.75 mM AMP or 0.005 mM ADP nor addition of up to 1.5 mM phosphate led to a reduced reaction rate
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additional information
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poor inhibition by adenosine and UTP, no inhibition by cytidine, guanosine, uridine, CMP, CTP, GTP, cGMP, and UMP
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additional information
discovery and synthesis of analogues of lead compound allosteric inhibitor (2,4-bis(aziridin-1-yl)-6-(1-phenylpyrrol-2-yl)-S-triazine) as inhibitors of bacterial PPiases
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additional information
-
discovery and synthesis of analogues of lead compound allosteric inhibitor (2,4-bis(aziridin-1-yl)-6-(1-phenylpyrrol-2-yl)-S-triazine) as inhibitors of bacterial PPiases
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additional information
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the enzyme is inhibited by phosphorylation
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additional information
C-substituted derivatives of methylene bisphosphonate, which are nonhydrolyzable diphosphate analogues, bind to Family II PPases 2-3 orders of magnitude more weakly than to Family I enzymes, whereas PNP binds with similar affinity, regardless of the metal cofactor bound
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additional information
addition of EDTA up to 0.5 mM to the assay mixture does not result in any change in the PPase activity
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additional information
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the enzyme is not inhibited by Na+
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