Activating Compound | Comment | Organism | Structure |
---|---|---|---|
1-[1-(ethylsulfonyl)-2,3-dihydro-1H-indol-5-yl]-2-[(4-methoxyphenyl)sulfanyl]ethanone | - |
Homo sapiens | |
2,3-dihydro-1,4-benzodioxin-6-yl[2-methyl-1-(methylsulfonyl)-2,3-dihydro-1H-indol-5-yl]methanone | - |
Homo sapiens | |
2,6-difluorophenyl 5-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-2-methyl-2,3-dihydro-1H-indole-1-sulfonate | - |
Homo sapiens | |
2-((2,3-dihydrobenzo[b][1,4]dioxin-6-yl)thio)-1-(2-methyl-1-(methylsulfonyl)indolin-5-yl) ethanone | - |
Homo sapiens | |
2-(2,3-dihydro-1,4-benzodioxin-6-ylsulfanyl)-1-[2-methyl-1-(methylsulfonyl)-2,3-dihydro-1H-indol-5-yl]ethanone | - |
Homo sapiens | |
2-(3,4-dihydro-2H-1,5-benzodioxepin-7-ylsulfanyl)-1-[1-(ethylsulfonyl)-2,3-dihydro-1H-indol-5-yl]ethanone | - |
Homo sapiens | |
2-[(3,5-difluorophenyl)sulfanyl]-1-[1-(ethylsulfonyl)-2,3-dihydro-1H-indol-5-yl]ethanone | - |
Homo sapiens | |
3-fluorophenyl 5-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-2,3-dihydro-1H-indene-1-sulfonate | - |
Homo sapiens | |
3-methoxyphenyl 5-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-2-methyl-2,3-dihydro-1H-indole-1-sulfonate | - |
Homo sapiens | |
4-fluorophenyl 5-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-2-methyl-2,3-dihydro-1H-indole-1-sulfonate | - |
Homo sapiens | |
5-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-1-(methylsulfonyl)-1H-indole | - |
Homo sapiens | |
5-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-2-methyl-1-(methylsulfonyl)-2,3-dihydro-1H-indole | - |
Homo sapiens | |
5-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-2-methyl-1-(phenylsulfonyl)-2,3-dihydro-1H-indole | - |
Homo sapiens | |
5-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-3-methyl-1-(methylsulfonyl)-1H-indole | - |
Homo sapiens | |
6-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-1-(methylsulfonyl)-1,2,3,4-tetrahydroquinoline | - |
Homo sapiens | |
6-{hydroxy[1-(methylsulfonyl)-1,2,3,7a-tetrahydro-5H-inden-5-ylidene]oxido-l6-sulfanyl}-2,3-dihydro-1,4-benzodioxine | - |
Homo sapiens | |
6-{[1-(cyclopropylsulfonyl)-2,3-dihydro-1H-inden-5-yl]sulfonyl}-2,3-dihydro-1,4-benzodioxine | - |
Homo sapiens | |
6-{[1-(ethylsulfonyl)-2,3-dihydro-1H-inden-5-yl]sulfonyl}-2,3-dihydro-1,4-benzodioxine | - |
Homo sapiens | |
6-{[1-(methylsulfonyl)-2,3-dihydro-1H-inden-5-yl]sulfonyl}-2,3-dihydro-1,4-benzodioxine | - |
Homo sapiens | |
6-{[1-(phenylsulfonyl)-2,3-dihydro-1H-inden-5-yl]sulfonyl}-2,3-dihydro-1,4-benzodioxine | - |
Homo sapiens | |
6-{[2-(ethylsulfonyl)-2,3-dihydro-1H-inden-5-yl]sulfonyl}-2,3-dihydro-1,4-benzodioxine | - |
Homo sapiens | |
6-{[2-(methylsulfonyl)-2,3-dihydro-1H-inden-5-yl]sulfonyl}-2,3-dihydro-1,4-benzodioxine | - |
Homo sapiens | |
6-{[2-(phenylsulfonyl)-2,3-dihydro-1H-inden-5-yl]sulfonyl}-2,3-dihydro-1,4-benzodioxine | - |
Homo sapiens | |
6-{[2-(tert-butylsulfonyl)-2,3-dihydro-1H-inden-5-yl]sulfonyl}-2,3-dihydro-1,4-benzodioxine | - |
Homo sapiens | |
additional information | 1-(sulfonyl)-5-(arylsulfonyl)indoline as activators of the tumor cell specific M2 isoform of pyruvate kinase, synthesis, structure-activity relationship analysis, enzyme active site docking, enzymatic reaction kinetics, selectivity, and pharmaceutical properties, overview. Activating potencies of the compounds compared for isozymes PKM2 and PKM1 | Homo sapiens | |
N-(2,3-dihydro-1,4-benzodioxin-6-yl)-2-methyl-1-(methylsulfonyl)-2,3-dihydro-1H-indole-5-sulfonamide | - |
Homo sapiens | |
N-[2-methyl-1-(methylsulfonyl)-2,3-dihydro-1H-indol-5-yl]-2,3-dihydro-1,4-benzodioxine-6-sulfonamide | - |
Homo sapiens | |
N-[4-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-3-methylphenyl]-N-ethylmethanesulfonamide | - |
Homo sapiens | |
N-[4-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)phenyl]-N-(propan-2-yl)methanesulfonamide | - |
Homo sapiens | |
N-[4-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)phenyl]-N-ethylmethanesulfonamide | - |
Homo sapiens | |
N-{4-[(2,3-dihydro-1,4-benzodioxin-6-ylsulfanyl)acetyl]phenyl}methanesulfonamide | - |
Homo sapiens | |
phenyl 5-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-2-methyl-2,3-dihydro-1H-indole-1-sulfonate | - |
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 + pyruvate | Homo sapiens | - |
ADP + phosphoenolpyruvate | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
additional information | prevalence of PKM2 in cancer cells relative to the prevalence of PKM1 in many norma cells | Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + pyruvate | - |
Homo sapiens | ADP + phosphoenolpyruvate | - |
? |
Synonyms | Comment | Organism |
---|---|---|
PKM1 | - |
Homo sapiens |
PKM2 | - |
Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
ATP | - |
Homo sapiens |
General Information | Comment | Organism |
---|---|---|
physiological function | the Warburg effect, a metabolic change, originates from a shift in the expression of alternative spliced isoforms of the glycolytic enzyme pyruvate kinase, from PKM1 to PKM2. While PKM1 is constitutively active, PKM2 is switched from an inactive dimer form to an active tetramer form by small molecule activators. Activation of PKM2 may counter the abnormal cellular metabolism in cancer cells, and consequently decreased cellular proliferation | Homo sapiens |