| + |
EGFR | up-regulates activity 
phosphorylation
|
KCNN1 |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-276490 |
Tyr109 |
KRKRLSDyALIFGMF |
Homo sapiens |
HEK-293 Cell |
| pmid |
sentence |
| 23496660 |
These results demonstrate the novel information that hSKCa1 channels are inhibited by genistein, T25 and AG556 via EGFR tyrosine kinase inhibition, which is related to the phosphorylation of Tyr(109) in the N-terminus. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
Naphtho[1,2-d]thiazol-2-amine | up-regulates activity
chemical activation
|
KCNN1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258026 |
|
|
Homo sapiens |
HEK-293 Cell |
| pmid |
sentence |
| 18955585 |
Here, we used the neuroprotectant riluzole as a template for the design of KCa2/3 channel activators that are potent enough for in vivo studies. Of a library of 41 benzothiazoles, we identified 2 compounds, anthra[2,1-d]thiazol-2-ylamine (SKA-20) and naphtho[1,2-d]thiazol-2-ylamine (SKA-31), which are 10 to 20 times more potent than riluzole and activate KCa2.1 with EC50 values of 430 nM and 2.9 μM, KCa2.2 with an EC50 value of 1.9 μM, KCa2.3 with EC50 values of 1.2 and 2.9 μM, and KCa3.1 with EC50 values of 115 and 260 nM. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
Anthra[2,1-d]thiazol-2-ylamine | up-regulates activity
chemical activation
|
KCNN1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258023 |
|
|
Homo sapiens |
HEK-293 Cell |
| pmid |
sentence |
| 18955585 |
Here, we used the neuroprotectant riluzole as a template for the design of KCa2/3 channel activators that are potent enough for in vivo studies. Of a library of 41 benzothiazoles, we identified 2 compounds, anthra[2,1-d]thiazol-2-ylamine (SKA-20) and naphtho[1,2-d]thiazol-2-ylamine (SKA-31), which are 10 to 20 times more potent than riluzole and activate KCa2.1 with EC50 values of 430 nM and 2.9 μM, KCa2.2 with an EC50 value of 1.9 μM, KCa2.3 with EC50 values of 1.2 and 2.9 μM, and KCa3.1 with EC50 values of 115 and 260 nM. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
Riluzole | up-regulates activity
chemical activation
|
KCNN1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258021 |
|
|
Homo sapiens |
HEK-293 Cell |
| pmid |
sentence |
| 18955585 |
Here, we used the neuroprotectant riluzole as a template for the design of KCa2/3 channel activators that are potent enough for in vivo studies. Of a library of 41 benzothiazoles, we identified 2 compounds, anthra[2,1-d]thiazol-2-ylamine (SKA-20) and naphtho[1,2-d]thiazol-2-ylamine (SKA-31), which are 10 to 20 times more potent than riluzole and activate KCa2.1 with EC50 values of 430 nM and 2.9 μM, KCa2.2 with an EC50 value of 1.9 μM, KCa2.3 with EC50 values of 1.2 and 2.9 μM, and KCa3.1 with EC50 values of 115 and 260 nM. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
3.0
KCNN1
- 
- 