Literature summary for 2.7.11.10 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.

Search for more literature for 2.7.11.10

Application

Application	Comment	Organism
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)

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

Protein Variants

Protein Variants	Comment	Organism
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
F26A	site-directed mutagenesis, the mutant has lost the time-dependent binding of inhibitor PHA-408	Homo sapiens
F26W	site-directed mutagenesis	Homo sapiens
K106N	site-directed mutagenesis	Homo sapiens
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
M96L	site-directed mutagenesis	Homo sapiens
Y169F	site-directed mutagenesis, the mutant shows time-dependent inhibition by PHA-408 like the wild-type	Homo sapiens

Inhibitors

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

Metals/Ions

Metals/Ions	Comment	Organism	Structure
Mg2+	required	Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates	Organism	Comment (Nat. Sub.)	Natural Products	Comment (Nat. Pro.)	Rev.	Reac.
ATP + [IkappaB protein]	Homo sapiens	-	ADP + [IkappaB phosphoprotein]	-	?

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	O14920	-	-

Purification (Commentary)

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

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
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]	-	?
ATP + [IkappaB protein]	-	Homo sapiens	ADP + [IkappaB phosphoprotein]	-	?

Synonyms

Synonyms	Comment	Organism
IkappaB kinase-2	-	Homo sapiens
IKK-2	-	Homo sapiens

Temperature Optimum [°C]

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

pH Optimum

pH Optimum Minimum	pH Optimum Maximum	Comment	Organism
7.6	-	aassay at	Homo sapiens

Cofactor

Cofactor	Comment	Organism	Structure
ATP	-	Homo sapiens

General Information

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

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Release 2023.1 (January 2023)