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Literature summary for 2.7.1.91 extracted from

  • Gao, P.; Peterson, Y.; Smith, R.; Smith, C.
    Characterization of isoenzyme-selective inhibitors of human sphingosine kinases (2012), PLoS ONE, 7, e44543.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.7.1.91

Cloned(Commentary)

Cloned (Comment) Organism
transfection of A498 kidney adenocarcinoma cells Homo sapiens

Crystallization (Commentary)

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

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

Organism UniProt Comment Textmining
Homo sapiens Q9NRA0 isoform SK2
-
Homo sapiens Q9NYA1 isoform SK1
-

Ki Value [mM]

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

Expression

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