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2.7.1.138: ceramide kinase

This is an abbreviated version!
For detailed information about ceramide kinase, go to the full flat file.

Word Map on EC 2.7.1.138

Reaction

ATP
+
ceramide
=
ADP
 +
ceramide 1-phosphate

Synonyms

acylsphingosine kinase, ceramide kinase, CERK, DCERK protein, hCERK, kinase, acylsphingosine (phosphorylating), More

ECTree

     2 Transferases
         2.7 Transferring phosphorus-containing groups
             2.7.1 Phosphotransferases with an alcohol group as acceptor
                2.7.1.138 ceramide kinase

Inhibitors

Inhibitors on EC 2.7.1.138 - ceramide kinase

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(4aR,6aS,12aS,12bR)-10-hydroxy-4,4,6a,12b-tetramethyl-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H-benzo(a)xanthene-8,11-dione
-
KD, enantiomer of K1, strongly inhibits CerK activity
(4aS,6aR,12aR,12bS)-10-hydroxy-4,4,6a,12b-tetramethyl-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H-benzo(a)xanthene-8,11-dione
1alpha,25-dihydroxyvitamin D3
enzyme activity decreases by approximately 40% in the presence of the hormone
2,5-dihydroxy-3-(((1R,4aR,8aR)-5,5,8a-trimethyl-2-methylidenedecahydronaphthalen-1-yl)methyl)cyclohexa-2,5-diene-1,4-dione
-
KB, enantiomer of K1, strongly inhibits CerK activity
2,5-dihydroxy-3-(((1S,2S,4aS,8aR)-2,5,5,8a-tetramethyldecahydronaphthalen-1-yl)methyl)cyclohexa-2,5-diene-1,4-dione
-
KC, F12509A with an additional hydrogen at the double bond in methylene position, weak inhibition
2,5-dihydroxy-3-(((1S,4aS,8aS)-5,5,8a-trimethyl-2-methylidenedecahydronaphthalen-1-yl)methyl)cyclohexa-2,5-diene-1,4-dione
-
F12509A, inhibitor of sphingosine kinase 1, weak inhibition
2,5-dihydroxy-3-[[(4aS,8aS)-2,5,5,8a-tetramethyl-3,4,4a,5,6,7,8,8a-octahydronaphthalen-1-yl]methyl]cyclohexa-2,5-diene-1,4-dione
-
K1, novel F-12509A olefin isomer, inhibitor decreases ceramide 1-phosphate levels without changing other lipids such as ceramide and sphingomyelin
3,3-cholamidopropyl-dimethylammonio-1-propanesulfonate
almost complete inhibition at high concentrations
3-(cyclohexylmethyl)-2,5-dihydroxycyclohexa-2,5-diene-1,4-dione
-
K2, cyclohexane derivative with a benzoquinone, weak inhibition
adamantane-1-carboxylic acid (2-benzoylamino-benzothiazol-6-yl)amide
-
NVP-231, a potent, specific, and reversible CerK inhibitor that competitively inhibits binding of ceramide to CerK
all-trans retinoic acid
inhibits ceramide kinase transkription in neuroblastoma cells
C2-ceramide
-
-
Ca2+
above 1 mM; inhibition above 1 mM
ceramide kinase inhibitor K1
-
-
D-erythro-N,N-dimethylsphingosine
-
dimethylsphingosine
-
DMS
F-12509A
0.1 mM, 40-50% inhibition, sphingosine kinase inhibitor
KN-93
-
-
lauryldimethylammonium N-oxide
inhibitory at low concentrations
N,N-dimethylsphingosine
0.1 mM, 65% inhibition
N-acetyl-D-erythro-sphingenine
substrate inhibition above 0.1 mM
N-acetylsphingosine
-
i.e. C2-Cer, in vivo during inhibition of mast cell degranulation
N-ethyl-maleimide
thiol modifiying agent stops CerK acitivity, demonstrating that CerK contains exposed cysteine residues important for enzymatic activity
N-laurylsarcosine
inhibitory at low concentrations
N-[2-(benzoylamino)-6-benzothiazolyl]-tricyclo[3.3.1.13,7] decane-1-carboxamide
-
NVP-231
octyl-beta-D-glucopyranoside
almost complete inhibition at high concentrations
siRNA
-
sphinganine
-
sphingenine
-
sphingosine
0.1 mM, 55% inhibition
W-7
-
calmodulin antagonist
ZK191784
enzyme activity decreases by approximately 25% in the presence of the hormone analogue
additional information
-