Activating Compound | Comment | Organism | Structure |
---|---|---|---|
suramin | 0.01 mM, about 30% increase in activity of isoforms PTPalpha, LAR | Homo sapiens | |
tetrasodium 2-(((2-(3-(((3-(5-((2,5-disulfonatophenyl)carbamoyl)-1H-benzimidazol-2-yl)phenyl)carbamoyl)amino)phenyl)-1H-benzimidazol-5-yl)carbonyl)amino)benzene-1,4-disulfonate | 0.01 mM, up to 4.5 activation of isoform PTPalpha wild-type | Homo sapiens |
Protein Variants | Comment | Organism |
---|---|---|
416AA | of PTPalpha, Km-value similar to wild-type, up to 2fold activation by NF506 | Yersinia sp. |
416AA | of PTPalpha, Km-value similar to wild-type, up to 2fold activation by tetrasodium 2-(((2-(3-(((3-(5-((2,5-disulfonatophenyl)carbamoyl)-1H-benzimidazol-2-yl)phenyl)carbamoyl)amino)phenyl)-1H-benzimidazol-5-yl)carbonyl)amino)benzene-1,4-disulfonate | Homo sapiens |
529AA | of PTPalpha, Km-value similar to wild-type, up to 11.6fold activation by NF506 | Yersinia sp. |
529AA | of PTPalpha, Km-value similar to wild-type, up to 11.6fold activation by tetrasodium 2-(((2-(3-(((3-(5-((2,5-disulfonatophenyl)carbamoyl)-1H-benzimidazol-2-yl)phenyl)carbamoyl)amino)phenyl)-1H-benzimidazol-5-yl)carbonyl)amino)benzene-1,4-disulfonate | Homo sapiens |
G496V | of PTPalpha, 70% increase in Km-value, up to 13.5fold activation by NF506 | Yersinia sp. |
G496V | of PTPalpha, 70% increase in Km-value, up to 13.5fold activation by tetrasodium 2-(((2-(3-(((3-(5-((2,5-disulfonatophenyl)carbamoyl)-1H-benzimidazol-2-yl)phenyl)carbamoyl)amino)phenyl)-1H-benzimidazol-5-yl)carbonyl)amino)benzene-1,4-disulfonate | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
disodium 3-(((4-methyl-3-(((2-methyl-5-((3-sulfonatophenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)benzenesulfonate | suramin-derivative, 50% inhibition at 0.030 mM, reversible and competitive | Yersinia sp. | |
disodium 4-(((4-methyl-3-(((3-(((3-((2-methyl-5-((4-sulfonatophenyl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)benzenesulfonate | suramin-derivative, 50% inhibition of PTP1B at 0.010 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR | Homo sapiens | |
disodium 4-(((4-methyl-3-(((3-(((3-((2-methyl-5-((4-sulfonatophenyl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)benzenesulfonate | suramin-derivative, 50% inhibition at 0.012mM, reversible and competitive | Yersinia sp. | |
disodium hydrogen (3-(((4-(((4-((3-(hydroxyphosphinato)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)phosphonate | suramin-derivative, 50% inhibition of PTP1B at 0.0096 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR | Homo sapiens | |
disodium hydrogen (3-(((4-(((4-((3-(hydroxyphosphinato)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)phosphonate | suramin-derivative, 50% inhibition above 0.1 mM, reversible and competitive | Yersinia sp. | |
hexasodium 8,8'-(((2E)-1,4-dioxobut-2-ene-1,4-diyl)bis(iminobenzene-3,1-diylcarbonylimino(4-methylbenzene-3,1-diyl)carbonylimino))dinaphthalene-1,3,5-trisulfonate | suramin-derivative, 50% inhibition of PTP1B at 0.005 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR | Homo sapiens | |
hexasodium 8,8'-(((2E)-1,4-dioxobut-2-ene-1,4-diyl)bis(iminobenzene-3,1-diylcarbonylimino(4-methylbenzene-3,1-diyl)carbonylimino))dinaphthalene-1,3,5-trisulfonate | suramin-derivative, 50% inhibition at 0.008mM, reversible and competitive | Yersinia sp. | |
hexasodium 8,8'-(benzene-1,3-diylbis(carbonyliminobenzene-3,1-diylcarbonylimino(4-methylbenzene-3,1-diyl)carbonylimino))dinaphthalene-1,3,5-trisulfonate | suramin-derivative, 50% inhibition of PTP1B at 0.0023 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR | Homo sapiens | |
hexasodium 8,8'-(benzene-1,3-diylbis(carbonyliminobenzene-3,1-diylcarbonylimino(4-methylbenzene-3,1-diyl)carbonylimino))dinaphthalene-1,3,5-trisulfonate | suramin-derivative, 50% inhibition at 0.0015M, reversible and competitive | Yersinia sp. | |
hexasodium 8-(((2'-(((3'-((4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl)biphenyl-2-yl)carbamoyl)amino)biphenyl-4-yl)carbonyl)amino)naphthalene-1,3,5-trisulfonate | suramin-derivative, 50% inhibition of PTP1B at 0.070 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR | Homo sapiens | |
hexasodium 8-(((2'-(((3'-((4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl)biphenyl-2-yl)carbamoyl)amino)biphenyl-4-yl)carbonyl)amino)naphthalene-1,3,5-trisulfonate | suramin-derivative, 50% inhibition at 0.020 mM, reversible and competitive | Yersinia sp. | |
hexasodium 8-(((3-methyl-4-(((3-(((3-((2-methyl-4-((4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,3,5-trisulfonate | suramin-derivative, 50% inhibition of PTP1B at 0.0037 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR | Homo sapiens | |
hexasodium 8-(((3-methyl-4-(((3-(((3-((2-methyl-4-((4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,3,5-trisulfonate | suramin-derivative, 50% inhibition at 0.007 mM, reversible and competitive | Yersinia sp. | |
hexasodium 8-(((3-methyl-4-(((4-(((4-((4-((4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,3,5-trisulfonate | suramin-derivative, 50% inhibition of PTP1B at 0.0021 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR | Homo sapiens | |
hexasodium 8-(((3-methyl-4-(((4-(((4-((4-((4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,3,5-trisulfonate | suramin-derivative, 50% inhibition at 0.0028mM, reversible and competitive | Yersinia sp. | |
hexasodium 8-(((4-(((3-(((3-((4-((4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,3,5-trisulfonate | suramin-derivative, 50% inhibition of PTP1B at 0.0016 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR | Homo sapiens | |
hexasodium 8-(((4-(((3-(((3-((4-((4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,3,5-trisulfonate | suramin-derivative, 50% inhibition at 0.002mM, reversible and competitive | Yersinia sp. | |
hexasodium 8-(((4-(1-methylethyl)-3-(((3-(((3-((2-(1-methylethyl)-5-((4,5,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,4,5-trisulfonate | suramin-derivative, 50% inhibition of PTP1B at 0.009 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR | Homo sapiens | |
hexasodium 8-(((4-(1-methylethyl)-3-(((3-(((3-((2-(1-methylethyl)-5-((4,5,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,4,5-trisulfonate | suramin-derivative, 50% inhibition at 0.013M, reversible and competitive | Yersinia sp. | |
hexasodium 8-(((4-ethyl-3-(((3-(((3-((2-ethyl-5-((4,5,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,4,5-trisulfonate | suramin-derivative, 50% inhibition of PTP1B at 0.009 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR | Homo sapiens | |
hexasodium 8-(((4-ethyl-3-(((3-(((3-((2-ethyl-5-((4,5,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,4,5-trisulfonate | suramin-derivative, 50% inhibition at 0.011M, reversible and competitive | Yersinia sp. | |
hexasodium 8-(((4-tert-butyl-3-(((3-(((3-((2-tert-butyl-5-((4,5,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,4,5-trisulfonate | suramin-derivative, 50% inhibition of PTP1B at 0.007 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR | Homo sapiens | |
hexasodium 8-(((4-tert-butyl-3-(((3-(((3-((2-tert-butyl-5-((4,5,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,4,5-trisulfonate | suramin-derivative, 50% inhibition of PTP1B at 0.013M, reversible and competitive | Yersinia sp. | |
hexasodium 8-([[2-(3-[[(3-[5-[(4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl]-1H-benzimidazol-2-yl]phenyl)carbamoyl]amino]phenyl)-1H-benzimidazol-5-yl]carbonyl]amino)naphthalene-1,3,5-trisulfonate | suramin-derivative, 50% inhibition of PTP1B at 0.00049 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR | Homo sapiens | |
hexasodium 8-([[2-(3-[[(3-[5-[(4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl]-1H-benzimidazol-2-yl]phenyl)carbamoyl]amino]phenyl)-1H-benzimidazol-5-yl]carbonyl]amino)naphthalene-1,3,5-trisulfonate | suramin-derivative, 50% inhibition at 0.00009M, reversible and competitive | Yersinia sp. | |
additional information | inhibition data for isoforms CD45, Cdc25A, VHR; not inhibitory to PTP1B, CD45: disodium 3-(((4-methyl-3-(((2-methyl-5-((3-sulfonatophenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)benzenesulfonate | Homo sapiens | |
N-(3-formylphenyl)-3-(((3-((3-formylphenyl)carbamoyl)phenyl)carbamoyl)amino)benzamide | suramin-derivative, 50% inhibition of PTP1B above 0.1 mM, reversible and competitive. Not inhibitory to PTPalpha, CD45 or LAR | Homo sapiens | |
N-(3-formylphenyl)-3-(((3-((3-formylphenyl)carbamoyl)phenyl)carbamoyl)amino)benzamide | suramin-derivative, 50% inhibition above 0.1 mM, reversible and competitive | Yersinia sp. | |
suramin | 50% inhibition of PTP1B at 0.011 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR | Homo sapiens | |
suramin | 50% inhibition at 0.007M, reversible and competitive | Yersinia sp. | |
tetrasodium 2-(((2-(3-(((3-(5-((2,5-disulfonatophenyl)carbamoyl)-1H-benzimidazol-2-yl)phenyl)carbamoyl)amino)phenyl)-1H-benzimidazol-5-yl)carbonyl)amino)benzene-1,4-disulfonate | suramin-derivative, 50% inhibition of PTP1B at 0.00025 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR | Homo sapiens | |
tetrasodium 2-(((2-(3-(((3-(5-((2,5-disulfonatophenyl)carbamoyl)-1H-benzimidazol-2-yl)phenyl)carbamoyl)amino)phenyl)-1H-benzimidazol-5-yl)carbonyl)amino)benzene-1,4-disulfonate | suramin-derivative, 50% inhibition at 0.0007mM, reversible and competitive | Yersinia sp. | |
tetrasodium 4,4'-(benzene-1,3-diylbis(carbonylimino))dinaphthalene-2,6-disulfonate | suramin-derivative, 50% inhibition of PTP1B above 0.1 mM, reversible and competitive. Not inhibitory to PTPalpha, CD45 or LAR | Homo sapiens | |
tetrasodium 4,4'-(benzene-1,3-diylbis(carbonylimino))dinaphthalene-2,6-disulfonate | suramin-derivative, 50% inhibition above 0.1 mM, reversible and competitive | Yersinia sp. | |
tetrasodium 4,4'-(benzene-1,3-diylbis(carbonyliminobenzene-4,1-diylcarbonylimino))dinaphthalene-2,6-disulfonate | suramin-derivative, 50% inhibition of PTP1B at 0.08 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR | Homo sapiens | |
tetrasodium 4,4'-(benzene-1,3-diylbis(carbonyliminobenzene-4,1-diylcarbonylimino))dinaphthalene-2,6-disulfonate | suramin-derivative, 50% inhibition at 0.045 mM, reversible and competitive | Yersinia sp. | |
tetrasodium 4-(((3-(((3,5-bis((4-sulfonatophenyl)carbamoyl)phenyl)carbamoyl)amino)-5-((4-sulfonatophenyl)carbamoyl)phenyl)carbonyl)amino)benzenesulfonate | suramin-derivative, 50% inhibition of PTP1B at 0.0045 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR | Homo sapiens | |
tetrasodium 4-(((3-(((3,5-bis((4-sulfonatophenyl)carbamoyl)phenyl)carbamoyl)amino)-5-((4-sulfonatophenyl)carbamoyl)phenyl)carbonyl)amino)benzenesulfonate | suramin-derivative, 50% inhibition at 0.005mM, reversible and competitive | Yersinia sp. | |
tetrasodium 4-(((3-(((5-((4,8-disulfonatonaphthalen-1-yl)carbamoyl)-2-methylphenyl)carbamoyl)amino)-4-methylphenyl)carbonyl)amino)naphthalene-1,5-disulfonate | suramin-derivative, 50% inhibition of PTP1B at 0.070 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR | Homo sapiens | |
tetrasodium 4-(((3-(((5-((4,8-disulfonatonaphthalen-1-yl)carbamoyl)-2-methylphenyl)carbamoyl)amino)-4-methylphenyl)carbonyl)amino)naphthalene-1,5-disulfonate | suramin-derivative, 50% inhibition at 0.0042 mM, reversible and competitive | Yersinia sp. |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
2.8 | - |
4-nitrophenyl phosphate | mutant 416AA, PTPalpha, 25°C, pH 7.0 | Homo sapiens | |
2.9 | - |
4-nitrophenyl phosphate | mutant 529AA, PTPalpha, 25°C, pH 7.0 | Homo sapiens | |
2.9 | - |
4-nitrophenyl phosphate | wild-type PTPalpha, 25°C, pH 7.0 | Homo sapiens | |
4.6 | - |
4-nitrophenyl phosphate | mutant G496V, PTPalpha, 25°C, pH 7.0 | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
isoforms PTP1B, CD45, PTPalpha, LAR | - |
Yersinia sp. | - |
isoform YOP | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
4-nitrophenyl phosphate + H2O | - |
Homo sapiens | 4-nitrophenol + phosphate | - |
? | |
4-nitrophenyl phosphate + H2O | - |
Yersinia sp. | 4-nitrophenol + phosphate | - |
? |
Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.77 | - |
4-nitrophenyl phosphate | mutant 416AA, PTPalpha, 25°C, pH 7.0 | Homo sapiens | |
1.25 | - |
4-nitrophenyl phosphate | mutant 529AA, PTPalpha, 25°C, pH 7.0 | Homo sapiens | |
1.26 | - |
4-nitrophenyl phosphate | wild-type PTPalpha, 25°C, pH 7.0 | Homo sapiens | |
1.74 | - |
4-nitrophenyl phosphate | mutant G496V, PTPalpha, 25°C, pH 7.0 | Homo sapiens |