Cloned (Comment) | Organism |
---|---|
gene ITPKA, recombinant expression in Escherichia coli strain BL21 | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
7-methylsulfanyl-3-phenyl-[1,3,4]thiadiazolo[2,3-c][1,2,4]triazin-4-one | 55% inhibition at 0.04 mM | Homo sapiens | |
additional information | in order to inhibit the metastasis-promoting activity of ITPKA, both its actin bundling and its InsP3kinase activity has to be blocked, inhibitor library screening, overview | Homo sapiens | |
N-(1,2-benzoxazol-3-yl)-4-methylbenzamide | 68% inhibition at 0.04 mM, mixed type inhibitor, that is nearly completely taken up by H1299 cells and remains stable after cellular uptake, the compound exhibits a robust stability and a high membrane permeability. The inhibitor provides the possibility to partly inhibit the metastasis-promoting effect of ITPKA in lung tumor cells. Inhibition mechanism of BAMB-4, overview | Homo sapiens | |
N-(4-ethoxyphenyl)pyrazolo[1,5-a]pyridine-3-carboxamide | 87% inhibition at 0.04 mM | Homo sapiens |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | Michaelis-Menten kinetics | Homo sapiens |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Mg2+ | required | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + 1D-myo-inositol 1,4,5-trisphosphate | Homo sapiens | - |
ADP + 1D-myo-inositol 1,3,4,5-tetrakisphosphate | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P23677 | isozyme/gene ITPKA | - |
Purification (Comment) | Organism |
---|---|
recombinant isozyme ITPKA from Escherichia coli strain BL21 by phosphocellulose chromatography and calmodulin affinity chromatography | Homo sapiens |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
carcinoma cell | - |
Homo sapiens | - |
H-1299 cell | - |
Homo sapiens | - |
neuron | neuron-specific isozyme | Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + 1D-myo-inositol 1,4,5-trisphosphate | - |
Homo sapiens | ADP + 1D-myo-inositol 1,3,4,5-tetrakisphosphate | - |
? |
Synonyms | Comment | Organism |
---|---|---|
inositol-1,4,5-trisphosphate-3-kinase A | - |
Homo sapiens |
ITPKA | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
30 | - |
assay at | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.5 | - |
assay at | Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
ATP | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.017 | - |
pH 7.5, 30°C, recombinant enzyme | Homo sapiens | N-(4-ethoxyphenyl)pyrazolo[1,5-a]pyridine-3-carboxamide | |
0.036 | - |
pH 7.5, 30°C, recombinant enzyme | Homo sapiens | 7-methylsulfanyl-3-phenyl-[1,3,4]thiadiazolo[2,3-c][1,2,4]triazin-4-one | |
0.037 | - |
pH 7.5, 30°C, recombinant enzyme | Homo sapiens | N-(1,2-benzoxazol-3-yl)-4-methylbenzamide |
General Information | Comment | Organism |
---|---|---|
physiological function | ectopic expression of the neuron-specific inositol-1,4,5-trisphosphate-3-kinase A in lung cancer cells increases their metastatic potential because the protein exhibits two actin regulating activities. The isozyme ITPKA bundles actin filaments and regulates inositol-1,4,5-trisphosphate (InsP3)-mediated calcium signals by phosphorylating InsP3 | Homo sapiens |