Cloned (Comment) | Organism |
---|---|
recombinant expression of GST-tagged enzyme in Escherichia coli strain BL21-CodonPlus(DE3) | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
3-(1-(2-morpholinoethyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione | - |
Homo sapiens | |
3-(1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione | - |
Homo sapiens | |
3-(1-(3-(piperidin-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione | - |
Homo sapiens | |
3-(1-(3-hydroxypropyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione | - |
Homo sapiens | |
3-(1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-1,2,4-triazol-1-yl)-1H-pyrrole-2,5-dione | - |
Homo sapiens | |
3-(1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione | - |
Homo sapiens | |
3-(1-(4-morpholinobutyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione | - |
Homo sapiens | |
3-(1-methyl-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione | - |
Homo sapiens | |
3-(1H-imidazol-1-yl)-4-(1-(3-morpholinopropyl)-1H-indol-3-yl)-1H-pyrrole-2,5-dione | - |
Homo sapiens | |
3-(1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione | - |
Homo sapiens | |
3-(5-methoxy-1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione | - |
Homo sapiens | |
3-(6-bromo-1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione | - |
Homo sapiens | |
3-(6-chloro-1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione | - |
Homo sapiens | |
3-(6-fluoro-1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1Hpyrrol-3-yl)-1H-pyrrole-2,5-dione | - |
Homo sapiens | |
3-(imidazo[1,2-a]pyridin-3-yl)-4-[2-(morpholine-4-carbonyl)-1,2,3,4-tetrahydro[1,4]diazepino[6,7,1-hi]indol-7-yl]-1H-pyrrole-2,5-dione | an imidazo[1,2-a]pyridinylindolylmaleimide | Homo sapiens | |
3-(naphthalen-1-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione | - |
Homo sapiens | |
3-phenyl-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione | - |
Homo sapiens | |
GF 109203X | a benzofuranylindolylmaleimide | Homo sapiens | |
additional information | design, synthesis, and evaluation of 3-aryl-4-pyrrolyl-maleimides as glycogen synthase kinase-3beta inhibitors. Compounds 3-(1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione, 3-(1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione, 3-(6-fluoro-1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1Hpyrrol-3-yl)-1H-pyrrole-2,5-dione, 3-(1-(3-hydroxypropyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione, and 3-(1-methyl-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione significantly reduce amyloidbeta-induced Tau hyperphosphorylation, showing the inhibition of GSK-3beta at the cellular level. Structure-activity relationships, in silico molecular modeling study, overview | Homo sapiens | |
Ro 31-8220 | a benzofuranylindolylmaleimide | Homo sapiens | |
staurosporine | a benzofuranylindolylmaleimide | 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 + [tau-protein] | Homo sapiens | - |
ADP + O-phospho-[tau-protein] | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P49841 | - |
- |
Purification (Comment) | Organism |
---|---|
recombinant GST-tagged enzyme from Escherichia coli strain BL21-CodonPlus(DE3) by glutathione affinity chromatography and tag cleavage by thrombin | Homo sapiens |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
neuroblastoma cell | - |
Homo sapiens | - |
SH-SY5Y cell | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + [tau-protein] | - |
Homo sapiens | ADP + O-phospho-[tau-protein] | - |
? |
Synonyms | Comment | Organism |
---|---|---|
glycogen synthase kinase-3beta | - |
Homo sapiens |
GSK-3beta | - |
Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
ATP | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.000028 | - |
pH and temperature not specified in the publication | Homo sapiens | staurosporine | |
0.0001 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-(1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione | |
0.00015 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-(1-(3-hydroxypropyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione | |
0.00016 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-(6-fluoro-1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1Hpyrrol-3-yl)-1H-pyrrole-2,5-dione | |
0.00021 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-(1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione | |
0.00026 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-(1-methyl-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione | |
0.00036 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-(6-chloro-1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione | |
0.00053 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-(1-(4-morpholinobutyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione | |
0.00057 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-(5-methoxy-1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione | |
0.00101 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-(6-bromo-1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione | |
0.00129 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-(1-(3-(piperidin-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione | |
0.00192 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-(1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione | |
0.00204 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-(1H-imidazol-1-yl)-4-(1-(3-morpholinopropyl)-1H-indol-3-yl)-1H-pyrrole-2,5-dione | |
0.00424 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-phenyl-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione | |
0.00645 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-(1-(2-morpholinoethyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione | |
0.0116 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-(1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-1,2,4-triazol-1-yl)-1H-pyrrole-2,5-dione | |
0.01186 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-(naphthalen-1-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione |