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Literature summary extracted from

  • Tegeder, I.; Niederberger, E.; Schmidt, R.; Kunz, S.; Guehring, H.; Ritzeler, O.; Michaelis, M.; Geisslinger, G.
    Specific inhibition of IkB kinase reduces hyperalgesia in inflammatory and neuropathic pain models in rats (2004), J. Neurosci., 24, 1637-1645.
    View publication on PubMedView publication on EuropePMC

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.11.10 S1627 specific for the IKK complex, inhibits purified IKK in vitro with IC50 of 0.02 mM, inhibits IKK and NFkappaB nuclear translocation in vivo in umbilical vein endothelial cells and in rats, overview Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
2.7.11.10 cytosol
-
 Homo sapiens 5829
-
2.7.11.10 nucleus
-
 Homo sapiens 5634
-

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.7.11.10 Mg2+
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.11.10 ATP + [IkappaB protein] Homo sapiens
-
 ADP + [IkappaB phosphoprotein]
-
 ?
2.7.11.10 additional information Homo sapiens enzyme is responsible for NFkappaB activation, specific inhibition of IkB kinase reduces hyperalgesia in inflammatory and neuropathic pain models in male Sprague-Dawley rats ?
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.11.10 Homo sapiens
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.7.11.10 native IkappaBalpha kinase from HeLa S3 cells by ammonium sulfate fractionation, ultrafiltration, and gel filtration Homo sapiens

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.7.11.10 endothelial cell from umbilical vein Homo sapiens
-
2.7.11.10 HeLa-S3 cell
-
 Homo sapiens
-
2.7.11.10 umbilical vein
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.11.10 ATP + [IkappaB protein]
-
 Homo sapiens ADP + [IkappaB phosphoprotein]
-
 ?
2.7.11.10 ATP + [IkappaB protein] the enzyme is also active with a peptide derived from IkappaB protein spanning Ser32 and Ser36 which are phosphorylated Homo sapiens ADP + [IkappaB phosphoprotein]
-
 ?
2.7.11.10 additional information enzyme is responsible for NFkappaB activation, specific inhibition of IkB kinase reduces hyperalgesia in inflammatory and neuropathic pain models in male Sprague-Dawley rats Homo sapiens ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.7.11.10 IKK
-
 Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.7.11.10 25
-
 assay at Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.7.11.10 7.5
-
 assay at Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.11.10 ATP
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.11.10 0.02
-
 specific for the IKK complex, inhibits purified IKK in vitro with IC50 of 0.02 mM, inhibits IKK and NFkappaB nuclear translocation in vivo in umbilical vein endothelial cells and in rats, overview Homo sapiens S1627