+ |
PRKACA | down-regulates
phosphorylation
|
KCNN2 |
0.2 |
Identifier |
Residue |
Sequence |
Organism |
Cell Line |
SIGNOR-145028 |
Ser464 |
QAIHQLRsVKMEQRK |
Homo sapiens |
|
pmid |
sentence |
16513649 |
Mutagenesis and mass spectrometry studies identified four pka phosphorylation sites: ser465 (minor site) and three amino acid residues ser568, ser569, and ser570 (major sites) within the carboxyl-terminal region. pka activation decreased sk2 surface localization |
|
Identifier |
Residue |
Sequence |
Organism |
Cell Line |
SIGNOR-145032 |
Ser567 |
SSSRRRRsSSTAPPT |
Homo sapiens |
|
pmid |
sentence |
16513649 |
Mutagenesis and mass spectrometry studies identified four pka phosphorylation sites: ser465 (minor site) and three amino acid residues ser568, ser569, and ser570 (major sites) within the carboxyl-terminal region. pka activation decreased sk2 surface localization |
|
Identifier |
Residue |
Sequence |
Organism |
Cell Line |
SIGNOR-145040 |
Ser568 |
SSRRRRSsSTAPPTS |
Homo sapiens |
|
pmid |
sentence |
16513649 |
Mutagenesis and mass spectrometry studies identified four pka phosphorylation sites: ser465 (minor site) and three amino acid residues ser568, ser569, and ser570 (major sites) within the carboxyl-terminal region. pka activation decreased sk2 surface localization |
|
Identifier |
Residue |
Sequence |
Organism |
Cell Line |
SIGNOR-145044 |
Ser569 |
SRRRRSSsTAPPTSS |
Homo sapiens |
|
pmid |
sentence |
16513649 |
Mutagenesis and mass spectrometry studies identified four pka phosphorylation sites: ser465 (minor site) and three amino acid residues ser568, ser569, and ser570 (major sites) within the carboxyl-terminal region. pka activation decreased sk2 surface localization |
|
Publications: |
4 |
Organism: |
Homo Sapiens |
+ |
Riluzole | up-regulates activity
chemical activation
|
KCNN2 |
0.8 |
Identifier |
Residue |
Sequence |
Organism |
Cell Line |
SIGNOR-258020 |
|
|
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 |
+ |
Naphtho[1,2-d]thiazol-2-amine | up-regulates activity
chemical activation
|
KCNN2 |
0.8 |
Identifier |
Residue |
Sequence |
Organism |
Cell Line |
SIGNOR-258027 |
|
|
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 |