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Literature summary extracted from

  • Mathialagan, S.; Poda, G.I.; Kurumbail, R.G.; Selness, S.R.; Hall, T.; Reitz, B.A.; Weinberg, R.A.; Kishore, N.; Mbalaviele, G.
    Expression, purification and functional characterization of IkappaB kinase-2 (IKK-2) mutants (2010), Protein Expr. Purif., 72, 254-261.
    View publication on PubMed

Application

EC Number Application Comment Organism
2.7.11.10 drug development because of its central role in the overall NF-kappaB regulation, IKK-2 is a viable target for drug discovery Homo sapiens

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.7.11.10 expression of C-terminally FLAG-tagged wild-type and mutant IKK-2s Homo sapiens

Protein Variants

EC Number Protein Variants Comment Organism
2.7.11.10 D145A site-directed mutagenesis, the IKK-2 is devoid of kinase activity despite its ability to bind ATP with high affinity and is not phosphorylated at the T loop. mutant binds a diverse collection of inhibitors with comparable binding affinities to wild-type IKK-2, inhibition by PHA-408 is reduced compared to the wild-type enzyme Homo sapiens
2.7.11.10 F26A site-directed mutagenesis, the mutant has lost the time-dependent binding of inhibitor PHA-408 Homo sapiens
2.7.11.10 F26W site-directed mutagenesis Homo sapiens
2.7.11.10 K106N site-directed mutagenesis Homo sapiens
2.7.11.10 K106Q site-directed mutagenesis, the mutant shows time-dependent inhibition like the wild-type, inhibition by PHA-408 is slightly increased compared to the wild-type enzyme Homo sapiens
2.7.11.10 M96L site-directed mutagenesis Homo sapiens
2.7.11.10 Y169F site-directed mutagenesis, the mutant shows time-dependent inhibition by PHA-408 like the wild-type Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.11.10 1-(4-chlorophenyl)-4-ureido-1H-pyrazole-3-carboxamide i.e. SC-108 Homo sapiens
2.7.11.10 1-(benzo[d][1,3]dioxol-5-yl)-8-(3-chloroisonicotinamido)-4,5-dihydro-1H-benzo[g]indazole-3-carboxamide i.e. PHA-379 Homo sapiens
2.7.11.10 1-(benzo[d][1,3]dioxol-5-yl)-8-(5-chloro-2-(4-methylpiperazin-1-yl)isonicotinamido)-4,5-dihydro-1H-benzo-[g]indazole-3-carboxamide i.e. PHA-250 Homo sapiens
2.7.11.10 2-amino-6-(2-hydroxy-6-isobutoxyphenyl)-4-(piperidin-3-yl)nicotinonitrile i.e. PHA-535E Homo sapiens
2.7.11.10 5-((3-fluorophenyl)ethynyl)-2-ureidothiophene-3-carboxamide i.e. PHA-966 Homo sapiens
2.7.11.10 5-(4-fluorophenyl)-2-ureidothiophene-3-carboxamide i.e. SC-440 Homo sapiens
2.7.11.10 5-amino-2,30-bithiophene-4-carboxamide i.e. SC-514 Homo sapiens
2.7.11.10 additional information structure-based design of IKK-2 inhibitors based on induced-fit docking into the homology model, overview Homo sapiens
2.7.11.10 N1-(1,8-dimethylimidazo-[1,2-a]quinoxalin-4-yl)ethane-1,2-diamine i.e. PHA-068E Homo sapiens
2.7.11.10 PHA-408 a selective IKK-2 inhibitor, shows time-dependent binding to the enzyme Homo sapiens

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.7.11.10 Mg2+ required 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]
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.11.10 Homo sapiens O14920
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.7.11.10 recombinant C-terminally FLAG-tagged wild-type and mutant IKK-2s Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.11.10 ATP + [biotinylated IkappaBa peptide] i.e. biotin-Gly-Leu-Lys-Lys-Glu-Arg-Leu-Leu-Asp-Asp-Arg-His-Asp-Ser32-Gly-Leu-Asp-Ser36-Met-Lys-Asp-Glu-Glu Homo sapiens ADP + [biotinylated IkappaBa phosphopeptide]
-
 ?
2.7.11.10 ATP + [IkappaB protein]
-
 Homo sapiens ADP + [IkappaB phosphoprotein]
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.7.11.10 IkappaB kinase-2
-
 Homo sapiens
2.7.11.10 IKK-2
-
 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 7.6
-
 aassay at Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.11.10 ATP
-
 Homo sapiens

General Information

EC Number General Information Comment Organism
2.7.11.10 additional information homology molecular model of the IKK-2 kinase domain, overview Homo sapiens
2.7.11.10 physiological function IKK-2 plays a central role in the overall NF-kappaB regulation Homo sapiens