Cloned (Comment) | Organism |
---|---|
transfection of A498 kidney adenocarcinoma cells | Homo sapiens |
Crystallization (Comment) | Organism |
---|---|
homology modeling based of Staphylococcus aureus diacylglycerol kinase, PDB entry 2QV7, and docking of substrate sphinganine 1-phosphatre to the model con taining bound ADP | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(2S,3R,4E)-2-(dimethylamino)octadec-4-ene-1,3-diol | inhibits both isoforms SK1 and SK2. Treatment triples the levels of isoform SK1 mRNA, but only slightly increases isoform SK2 expression; inhibits both isoforms SK1 and SK2. Treatment triples the levels of isoform SK1 mRNA, but only slightly increases isoform SK2 expression | Homo sapiens | |
2-(4-hydroxyanilino)-4-(4-chlorophenyl)thiazole | inhibits both isoforms SK1 and SK2. Treatment increases mRNAs for both isoforms SK1 and SK2 by about 4fold; inhibits both isoforms SK1 and SK2. Treatment increases mRNAs for both isoforms SK1 and SK2 by about 4fold | Homo sapiens | |
5-(4-chlorophenyl)-N-(pyridin-4-ylmethyl)tricyclo[3.3.1.13,7]decane-2-carboxamide | selective inhibition of isoform SK2 | Homo sapiens | |
5-(4-chlorophenyl)-N-[2-(3,4-dihydroxyphenyl)ethyl]tricyclo[3.3.1.13,7]decane-2-carboxamide | inhibits both isoforms SK1 and SK2; inhibits both isoforms SK1 and SK2 | Homo sapiens | |
N-(3-chloro-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-N-cyclohexylacetamide | selective inhibition of isoform SK1 | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | Q9NRA0 | isoform SK2 | - |
Homo sapiens | Q9NYA1 | isoform SK1 | - |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.00028 | - |
N-(3-chloro-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-N-cyclohexylacetamide | pH not specified in the publication, temperature not specified in the publication | Homo sapiens | |
0.0031 | - |
5-(4-chlorophenyl)-N-[2-(3,4-dihydroxyphenyl)ethyl]tricyclo[3.3.1.13,7]decane-2-carboxamide | pH not specified in the publication, temperature not specified in the publication | Homo sapiens | |
0.0042 | - |
5-(4-chlorophenyl)-N-[2-(3,4-dihydroxyphenyl)ethyl]tricyclo[3.3.1.13,7]decane-2-carboxamide | pH not specified in the publication, temperature not specified in the publication | Homo sapiens | |
0.0079 | - |
2-(4-hydroxyanilino)-4-(4-chlorophenyl)thiazole | pH not specified in the publication, temperature not specified in the publication | Homo sapiens | |
0.0093 | - |
5-(4-chlorophenyl)-N-(pyridin-4-ylmethyl)tricyclo[3.3.1.13,7]decane-2-carboxamide | pH not specified in the publication, temperature not specified in the publication | Homo sapiens | |
0.014 | - |
(2S,3R,4E)-2-(dimethylamino)octadec-4-ene-1,3-diol | pH not specified in the publication, temperature not specified in the publication | Homo sapiens | |
0.016 | - |
2-(4-hydroxyanilino)-4-(4-chlorophenyl)thiazole | pH not specified in the publication, temperature not specified in the publication | Homo sapiens | |
0.016 | - |
(2S,3R,4E)-2-(dimethylamino)octadec-4-ene-1,3-diol | pH not specified in the publication, temperature not specified in the publication | Homo sapiens |
Organism | Comment | Expression |
---|---|---|
Homo sapiens | knockdown of isoform SK2 expression results in overexpression of isoform SK1 in several cell lines. Treatment with inhibitor (2S,3R,4E)-2-(dimethylamino)octadec-4-ene-1,3-diol triples the levels of isoform SK1 mRNA, but only slightly increases isoform SK2 expression. Treatment with inhibitor 2-(4-hydroxyanilino)-4-(4-chlorophenyl)thiazole increases mRNAs for both isoforms SK1 and SK2 by about 4fold | up |