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Literature summary 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

Cloned(Commentary)

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

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.1.91 (3S)-1-([4-[(5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)methyl]phenyl]methyl)pyrrolidin-3-ol
-
Homo sapiens
2.7.1.91 (3S)-N-[(1S)-1-[4-[5-(2-cyclohexylethyl)-1,2,4-oxadiazol-3-yl]phenyl]propyl]-3-hydroxy-L-prolinamide
-
Homo sapiens
2.7.1.91 1-[[4-(4-tert-butylphenoxy)-3-fluorophenyl]methyl]pyrrolidin-3-ol
-
Homo sapiens
2.7.1.91 PF-543 potent, selective, sphingosine-competitive isoform SphK1 inhibitor Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.7.1.91 0.017
-
ATP isoform SphK1, at pH 7.4 and 23°C Homo sapiens
2.7.1.91 0.084
-
ATP isoform SphK2, at pH 7.4 and 23°C Homo sapiens

Metals/Ions

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

Natural Substrates/ Products (Substrates)

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

Organism

EC Number Organism UniProt Comment Textmining
2.7.1.91 Homo sapiens Q9NRA0
-
-
2.7.1.91 Homo sapiens Q9NYA1
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.1.91 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
-
?
2.7.1.91 ATP + sphingosine
-
Homo sapiens ADP + sphingosine 1-phosphate
-
?
2.7.1.91 ATP + sphingosine-fluorescin
-
Homo sapiens ADP + sphingosine 1-phosphate
-
?

Synonyms

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

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
2.7.1.91 0.53
-
ATP isoform SphK2, at pH 7.4 and 23°C Homo sapiens
2.7.1.91 7
-
ATP isoform SphK1, at pH 7.4 and 23°C Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.7.1.91 0.0000043
-
PF-543 isoform SphK1, at pH 7.4 and 23°C Homo sapiens

kcat/KM [mM/s]

EC Number kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
2.7.1.91 6.3
-
ATP isoform SphK2, at pH 7.4 and 23°C Homo sapiens
2.7.1.91 410
-
ATP isoform SphK1, at pH 7.4 and 23°C Homo sapiens