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(2-anilinoethane-1,1-diyl)bis(phosphonic acid)
(2E)-2-[(4-nitrophenyl)methylidene]-4,4-diphosphonobutanoic acid
2-[2-amino-3-[(2-amino-3-[[(1S)-1-carboxy-2-(4-hydroxyphenyl)ethyl]amino]-3-oxopropyl)disulfanyl]propanamido]-3-(4-hydroxyphenyl)propanoic acid
treating the wild-type Escherichia coli with the inhibitor, at 0.050 mM, results in a metabolic fingerprint that is an almost identicalntical metabolic behavior to the ppk1 knockout mutant
6-(4-aminobenzamido)-5-[(E)-[1-(2-chloro-5-sulfophenyl)-5-hydroxy-3-methyl-1H-pyrazol-4-yl]diazenyl]naphthalene-2-sulfonic acid
treating the wild-type Escherichia coli with the inhibitor, at 0.050 mM, results in a metabolic fingerprint that is completely identical to that of ppk1 knockout mutant
ammonium hydrochloride
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50% inhibition at 200 mM
Ca2+
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1 mM, 10% inhibition
Cu2+
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0.1 mM, 92% inhibition, 1 mM, complete inhibition
ellagic acid
Q9S646
ellagic acid derivatives from Terminalia chebula increase the susceptibility of Pseudomonas aeruginosa to stress by inhibiting polyphosphate kinase, oveview. Ellagic acid derivatives completely inhibit PPK1 activity at 0.5 mg/ml. Ellagic acid derivatives-treated Pseudomonas aeruginosa cells show marked reduction in polyphosphate granules in cytosol. Ellagic acid derivatives from Terminalia chebula inhibit PPK1 expression and its activity and increase the sensitivity of Pseudomonas aeruginosa to desiccation and oxidative stress while reducing tolerance to piperacillin
G-quadruplex thrombin binding aptamer
binds to PPK2 with a KD of 870 nM, noncompetitive
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Guanidine HCl
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5 mM, 50% inhibition of polyphosphate synthesis
guanosine 5'-tetraphosphate
histone
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reverse reaction, strong, activates forward reaction in the presence of phosphate
hydrolyzed glycogen
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complete inhibition
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MnATP2-
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at high concentrations, above 0.6 mM, activating below
NH4Cl
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200 mM, approx. 50% inhibition of glycogen-bound polyphosphate kinase
NSC-30205
0.1 mM, inhibits more than 80%, cytotoxic to THP-1 macrophages with TC50 value 0.01 mM
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NSC-345647
0.1 mM, inhibits more than 80%, cytotoxic to THP-1 macrophages with TC50 value 0.005 mM
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NSC-35676
0.1 mM, inhibits more than 80%, non-cytotoxic to THP-1 cells even at 0.05 mM concentration
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NSC-9037
0.1 mM, inhibits more than 80%, non-cytotoxic to THP-1 cells even at 0.05 mM concentration
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phalloidin
a heptapeptide toxin from the mushroom Amanita phalloides, which binds tightly and specifically to polymerized actin, inhibits DdPPK2 and DdPPK1, the latter by 80% at 10 nM, the molar ratio of phalloidin to DdPPK1 of 10:15 results in complete inhibition of DdPPK1 activity
Sodium fluoride
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slight inhibition
threonyltyrosyl-N-[(1R)-1-[(3-aminopropyl)amino]-2-(carboxyoxy)-2-oxoethyl]serinamide
poor chemical inhibitor of PPK1, it shows a drop of approximately 20% in the WT biofilm formation ability
Zn2+
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0.1 mM, 67% inhibition, 1 mM, complete inhibition
[(2,3-dichloroanilino)methylene]bis(phosphonic acid)
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[(3,5-dichloroanilino)methylene]bis(phosphonic acid)
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[(3-aminoanilino)methylene]bis(phosphonic acid)
[(3-carbamimidamidoanilino)methylene]bis(phosphonic acid)
[(4-benzylanilino)methylene]bis(phosphonic acid)
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[2-(2,3-dichlorophenyl)-1-hydroxyethane-1,1-diyl]bis(phosphonic acid)
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[2-(3,4-dichlorophenyl)-1-hydroxyethane-1,1-diyl]bis(phosphonic acid)
[2-(3-chloroanilino)ethane-1,1-diyl]bis(phosphonic acid)
[2-(3-nitroanilino)ethane-1,1-diyl]bis(phosphonic acid)
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[2-[(1-amino-2-methylbutyl)(hydroxy)phosphoryl]ethyl]phosphonic acid
(2-anilinoethane-1,1-diyl)bis(phosphonic acid)
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(2-anilinoethane-1,1-diyl)bis(phosphonic acid)
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(2E)-2-[(4-nitrophenyl)methylidene]-4,4-diphosphonobutanoic acid
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(2E)-2-[(4-nitrophenyl)methylidene]-4,4-diphosphonobutanoic acid
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(NH4)2SO4
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40 mM, almost complete inhibition
(NH4)2SO4
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activation up to 100 mM; inhibition at higher concentrations; strong inhibition
(NH4)2SO4
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strong inhibition
ADP
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0.025 mM, 0.05 mM, 0.1 mM and 0.25 mM, 56%, 68%, 77% and 100% inhibition, respectively of polyphosphate synthesis in crude extracts
ADP
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0.08 mM, complete inhibition
ADP
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0.2 mM, complete inhibition
ADP
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50%, 70% and 93% inhibition at 0.08 mM, 0.15 mM and 0.2 mM ADP, respectively
ADP
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competitive inhibition
ADP
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substrate inhibition
ADP
Q9S646
product inhibition
ADP
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0.25 mM, approx. 50% inhibition, 1 mM, complete inhibition
ADP
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4 mM, product inhibition
ADP
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2 mM, 50% inhibition of glycogen-bound polyphosphate kinase; product inhibition, about 50% inhibition at 2 mM
AMP
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AMP
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at high concentrations
AMP
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15% and 70% inhibition of the forward reaction at AMP/ADP ratios of 1 and 10, respectiverly
ATP
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substrate inhibition, at high concentrations
ATP
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free form, above 0.008 mM
ATP
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20% substrate inhibition at 2.4 mM
Co2+
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1 mM, 40% inhibition
Co2+
complete inhibition; complete inhibition; complete inhibition
diphosphate
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weak inhibition
diphosphate
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1 mM, complete inhibition
diphosphate
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10 mM, 66% inhibition of polyphosphate synthesis, 75% inhibition of GTP synthesis
diphosphate
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1 mM, complete inhibition
EDTA
complete inhibition
EDTA
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10 mM, complete inhibition
EDTA
low inhibition; low inhibition
F-
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5 mM, complete inhibition
F-
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20 mM, complete inhibition
F-
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5 mM, 75% inhibition
F-
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10 mM, complete inhibition
F-
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20 mM, complete inhibition
F-
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2 mM, 25% inhibition of glycogen-bound polyphosphate kinase
GMP
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GMP
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competitive inhibition of polyphosphate 750 and GDP in guanosine 5'-tetraphosphate synthesis
guanosine 5'-tetraphosphate
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guanosine 5'-tetraphosphate
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guanosine 5'-tetraphosphate
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guanosine 5'-tetraphosphate
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KCl
inhibits PPK1 80% at 500 mM, but not PPK2
KCl
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50 mM, 50% inhibition
Mg2+
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8 mM, complete inhibition
Mg2+
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free form, above 6 mM, activating below
Mn2+
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weak inhibition at 10 mM Mg2+
Mn2+
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free form, above 2 mM, activating below
phosphate
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above 20 mM; activates in the presence of histone
phosphate
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5.5 mM and 11 mM, 33% and 49% inhibition of forward reaction
phosphate
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2 mM, 50% inhibition of glycogen-bound polyphosphate kinase; strong inhibition
Polyphosphate
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65 residues, competitive inhibition of polyphosphate 750 and GDP in guanosine 5'-tetraphosphate synthesis
Polyphosphate
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substrate inhibition at 2 mM
polyphosphate(4)
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short polyphosphates inhibit the enzyme by blocking the ADP binding pocket
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polyphosphate(4)
short polyphosphates inhibit the enzyme by blocking the ADP binding pocket
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[(3-aminoanilino)methylene]bis(phosphonic acid)
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[(3-aminoanilino)methylene]bis(phosphonic acid)
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[(3-carbamimidamidoanilino)methylene]bis(phosphonic acid)
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[(3-carbamimidamidoanilino)methylene]bis(phosphonic acid)
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[2-(3,4-dichlorophenyl)-1-hydroxyethane-1,1-diyl]bis(phosphonic acid)
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[2-(3,4-dichlorophenyl)-1-hydroxyethane-1,1-diyl]bis(phosphonic acid)
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[2-(3-chloroanilino)ethane-1,1-diyl]bis(phosphonic acid)
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[2-(3-chloroanilino)ethane-1,1-diyl]bis(phosphonic acid)
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[2-[(1-amino-2-methylbutyl)(hydroxy)phosphoryl]ethyl]phosphonic acid
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[2-[(1-amino-2-methylbutyl)(hydroxy)phosphoryl]ethyl]phosphonic acid
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additional information
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no inhibition by UMP and CMP
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additional information
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not inhibited by NaCl
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additional information
screening of low-molecular-weight organophosphorus inhibitors against polyphosphate kinases from Cytophaga hutchinsonii and Escherichia coli. For Cytophaga hutchinsonii PPK2, almost all active inhibitors belong to N-substituted alpha-aminobisphosphonic acids preferentially possessing an additional basic function
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additional information
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not inhibited by 2,4-dinitrophenol or potassium arsenate
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additional information
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not inhibited by 3',5'-adenosine monophosphate
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additional information
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MIC values of wild-type and mutant strain ExPEC for diverse antibiotics, i.e. beta-lactams cefotaxime, ceftazidime, ampicillin, cefazolin, tazobactam, and ticarcillin, glycopeptide vancomycin, aminoglycosides gentamicin, gentamicin sulfate, amikacin macrolide, erythromycin, quinolones norfloxacin and levofloxacin, sulfonamide trimethoprim, sulfadiazine nitrofurans macrodantin, and lipopeptde polymyxin B, overview. Biofilm-grown DELTAppk and wild-type cells are similarly tolerant and more tolerant than planktonic cells
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additional information
screening of low-molecular-weight organophosphorus inhibitors against polyphosphate kinases from Cytophaga hutchinsonii and Escherichia coli. For Escherichia coli PPK1, only individual compounds with a distinct scaffold and functional group arrangement show potency
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additional information
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not inhibited by bafilomycin A1 or a protonophore
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additional information
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not inhibited by KCl; not inhibited by NaCl; not inhibited by phosphate; not inhibited by polyphosphate
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additional information
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a G9-quadruplex DNA aptamer inhibits isoform PPK2 with an IC50 of 40 nM and exhibits noncompetitive inhibition kinetics
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additional information
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enzymatic hydrolysis of glycogen
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additional information
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a G9-quadruplex DNA aptamer inhibits isoform PPK2 with an IC50 of 105 nM and exhibits noncompetitive inhibition kinetics
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