Application | Comment | Organism |
---|---|---|
medicine | the STS inhibitors 3-sulfamoyloxy-N-propyl-16,17-seco-estra-1,3,5(10)-triene-16,17-imide and 3-sulfamoyloxy-N-(1-pyridin-3-ylmethyl)-16,17-seco-estra-1,3,5(10)-triene-16,17-imide are devoid of estrogenic activity and have therapeutic potential for the treatment of hormone-dependent breast cancer | Rattus norvegicus |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
3-sulfamoyloxy-N-(1''-pyridin-3''-ylmethyl)-16,17-seco-estra-1,3,5(10)-triene-16,17-imide | highly potent inhibitor, IC50: 1 nM, 18times more inhibitory than estrone-3-O-sulfamate, in vivo inhibition of STS | Rattus norvegicus | |
3-sulfamoyloxy-N-propyl-16,17-seco-estra-1,3,5(10)-triene-16,17-imide | highly potent inhibitor, IC50: 1 nM, 18times more inhibitory than estrone-3-O-sulfamate, in vivo inhibition of STS | Rattus norvegicus | |
estrone-3-O-sulfamate | - |
Rattus norvegicus |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Rattus norvegicus | - |
ovariectomised female Wistar rats | - |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
liver | - |
Rattus norvegicus | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
estrone sulfate + H2O | - |
Rattus norvegicus | estrone + sulfate | - |
? |
Synonyms | Comment | Organism |
---|---|---|
STS | - |
Rattus norvegicus |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at | Rattus norvegicus |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.000001 | - |
highly potent inhibitor, IC50: 1 nM, 18times more inhibitory than estrone-3-O-sulfamate, in vivo inhibition of STS | Rattus norvegicus | 3-sulfamoyloxy-N-propyl-16,17-seco-estra-1,3,5(10)-triene-16,17-imide | |
0.000001 | - |
highly potent inhibitor, IC50: 1 nM, 18times more inhibitory than estrone-3-O-sulfamate, in vivo inhibition of STS | Rattus norvegicus | 3-sulfamoyloxy-N-(1''-pyridin-3''-ylmethyl)-16,17-seco-estra-1,3,5(10)-triene-16,17-imide |