Application | Comment | Organism |
---|---|---|
medicine | estrone sulfatase inhibitors can be used as drugs for the treatment of estrogen-dependent breast cancer | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
6-oxo-8,9,10,11-tetrahydro-7H-cyclohepta-[c][1]benzopyran-3-O-sulfamate | 6,6,7-COUMATE, IC50: 5.1 nM in JEG-3 cells, 0.43 nM in MCF-7 cells | Homo sapiens | |
6-oxo-8,9,10,11-tetrahydro-7H-cyclohepta-[c][1]benzopyran-3-O-sulfamate | 6,6,7-COUMATE, potent inhibitor, in vivo inhibition study, more inhibitory than TX-1299 | Rattus norvegicus | |
estrone-3-sulfamate | best inhibitor, IC50: 3.2 nM in JEG-3 cells, 0.08 nM in MCF-7 cells | Homo sapiens | |
additional information | not inhibited by danazol or letrozole | Homo sapiens | |
TX-1299 | non-steroid Theramex compound, strong inhibitor, IC50: 5.3 nM in JEG-3 cells, 0.76 nM in MCF-7 cells | Homo sapiens | |
TX-1299 | non-steroid Theramex compound, potent inhibitor, in vivo inhibition study, 80% as inhibitory as 6,6,7-COUMATE | Rattus norvegicus | |
TX-1492 | non-steroid Theramex compound, strong inhibitor, IC50: 22.5 nM in JEG-3 cells, 0.07 nM in MCF-7 cells | Homo sapiens | |
TX-1506 | non-steroid Theramex compound, strong inhibitor, IC50: 11.9 nM in JEG-3 cells, 0.06 nM in MCF-7 cells | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Rattus norvegicus | - |
adult Wistar female ovariectomized rats | - |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
JEG-3 cell | choriocarcinoma cell, more than 80times higher enzyme activity than in MCF-7 cells | Homo sapiens | - |
MCF-7 cell | breast adenocarcinoma cell, more than 80times lower enzyme activity than in JEG-3 cells | Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
estrone sulfate + H2O | - |
Homo sapiens | estrone + sulfate | - |
? | |
estrone sulfate + H2O | - |
Rattus norvegicus | estrone + sulfate | - |
? |
Synonyms | Comment | Organism |
---|---|---|
estrone sulfatase | - |
Homo sapiens |
estrone sulfatase | - |
Rattus norvegicus |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00000006 | - |
non-steroid Theramex compound, strong inhibitor, 0.06 nM in MCF-7 cells | Homo sapiens | TX-1506 | |
0.00000008 | - |
IC50 0.08 nM in MCF-7 cells | Homo sapiens | estrone-3-sulfamate | |
0.00000043 | - |
IC50 0.43 nM in MCF-7 cells | Homo sapiens | 6-oxo-8,9,10,11-tetrahydro-7H-cyclohepta-[c][1]benzopyran-3-O-sulfamate | |
0.00000076 | - |
non-steroid Theramex compound, strong inhibitor, 0.76 nM in MCF-7 cells | Homo sapiens | TX-1299 | |
0.0000032 | - |
best inhibitor, IC50: 3.2 nM in JEG-3 cells | Homo sapiens | estrone-3-sulfamate | |
0.0000051 | - |
6,6,7-COUMATE, IC50: 5.1 nM in JEG-3 cells | Homo sapiens | 6-oxo-8,9,10,11-tetrahydro-7H-cyclohepta-[c][1]benzopyran-3-O-sulfamate | |
0.0000053 | - |
non-steroid Theramex compound, strong inhibitor, IC50: 5.3 nM in JEG-3 cells | Homo sapiens | TX-1299 | |
0.0000119 | - |
non-steroid Theramex compound, strong inhibitor, IC50: 11.9 nM in JEG-3 cells | Homo sapiens | TX-1506 | |
0.0000225 | - |
non-steroid Theramex compound, strong inhibitor, IC50: 22.5 nM in JEG-3 cells | Homo sapiens | TX-1492 |