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Literature summary for 2.7.1.91 extracted from

  • Kashem, M.; Kennedy, C.; Fogarty, K.; Dimock, J.; Zhang, Y.; Sanville-Ross, M.; Skow, D.; Brunette, S.; Swantek, J.; Hummel, H.; Swindle, J.; Nelson, R.
    A high-throughput genetic complementation assay in yeast cells identified selective inhibitors of sphingosine kinase 1 not found using a cell-free enzyme assay (2016), Assay Drug Dev. Technol., 14, 39-49 .
    View publication on PubMed
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Cloned(Commentary)

Cloned (Comment) Organism
isoform SphK1 is expressed in Saccharomyces cerevisiae strain CGY32 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(3S)-1-([4-[(5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)methyl]phenyl]methyl)pyrrolidin-3-ol
-
 Homo sapiens
(3S)-N-[(1S)-1-[4-[5-(2-cyclohexylethyl)-1,2,4-oxadiazol-3-yl]phenyl]propyl]-3-hydroxy-L-prolinamide
-
 Homo sapiens
1-[[4-(4-tert-butylphenoxy)-3-fluorophenyl]methyl]pyrrolidin-3-ol
-
 Homo sapiens
PF-543 potent, selective, sphingosine-competitive isoform SphK1 inhibitor Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.017
-
 ATP isoform SphK1, at pH 7.4 and 23°C Homo sapiens
0.084
-
 ATP isoform SphK2, at pH 7.4 and 23°C Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ required for activity Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + sphingosine Homo sapiens
-
 ADP + sphingosine 1-phosphate
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens Q9NRA0
-
-
Homo sapiens Q9NYA1
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + 7-nitro-2-1,3-benzoxadiazol-4-yl-labeled sphingosine
-
 Homo sapiens ADP + 7-nitro-2-1,3-benzoxadiazol-4-yl-labeled sphingosine 1-phosphate
-
 ?
ATP + sphingosine
-
 Homo sapiens ADP + sphingosine 1-phosphate
-
 ?
ATP + sphingosine-fluorescin
-
 Homo sapiens ADP + sphingosine 1-phosphate
-
 ?

Synonyms

Synonyms Comment Organism
sphingosine kinase 1
-
 Homo sapiens
sphingosine kinase 2
-
 Homo sapiens
SPHK1 isoform Homo sapiens
SPHK2 isoform Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.53
-
 ATP isoform SphK2, at pH 7.4 and 23°C Homo sapiens
7
-
 ATP isoform SphK1, at pH 7.4 and 23°C Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000043
-
 PF-543 isoform SphK1, at pH 7.4 and 23°C Homo sapiens

kcat/KM [mM/s]

kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
6.3
-
 ATP isoform SphK2, at pH 7.4 and 23°C Homo sapiens
410
-
 ATP isoform SphK1, at pH 7.4 and 23°C Homo sapiens