Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 2.7.1.138 extracted from

  • Kumada, H.; Mitsutake, S.; Inagaki, Y.; Mitsunaga, S.; Tsuchikawa, H.; Katsumura, S.; Igarashi, Y.
    Kinetics of the ceramide kinase inhibitor K1, a suppressor of mast-cell activation (2007), Biosci. Biotechnol. Biochem., 71, 2581-2584.
    View publication on PubMed
Search for more literature for 2.7.1.138

Application

Application Comment Organism
medicine potential target for anti-allergic therapeutics Rattus norvegicus

Inhibitors

Inhibitors Comment Organism Structure
(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 Rattus norvegicus
(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 K1, non-competitive, suppresses the activation of mast cells, strongly inhibits CerK activity Rattus norvegicus
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 Rattus norvegicus
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 Rattus norvegicus
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 Rattus norvegicus
3-(cyclohexylmethyl)-2,5-dihydroxycyclohexa-2,5-diene-1,4-dione K2, cyclohexane derivative with a benzoquinone, weak inhibition Rattus norvegicus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ceramide + ATP Rattus norvegicus CerK is involved in the regulation of mast cells ceramide 1-phosphate + ADP
-
 ?

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
mast cell
-
 Rattus norvegicus
-
RBL-2H3 cell
-
 Rattus norvegicus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ceramide + ATP
-
 Rattus norvegicus ceramide 1-phosphate + ADP
-
 ?
ceramide + ATP CerK is involved in the regulation of mast cells Rattus norvegicus ceramide 1-phosphate + ADP
-
 ?

Synonyms

Synonyms Comment Organism
CERK
-
 Rattus norvegicus

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0022
-
 (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
-
 Rattus norvegicus
0.0033
-
 (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
-
 Rattus norvegicus
0.452
-
 2,5-dihydroxy-3-(((1S,2S,4aS,8aR)-2,5,5,8a-tetramethyldecahydronaphthalen-1-yl)methyl)cyclohexa-2,5-diene-1,4-dione
-
 Rattus norvegicus