Literature summary for 2.7.11.10 extracted from

Lorenzo, P.; Alvarez, R.; Ortiz, M.A.; Alvarez, S.; Piedrafita, F.J.; de Lera, A.R.
Inhibition of IkappaB kinase-beta and anticancer activities of novel chalcone adamantyl arotinoids (2008), J. Med. Chem., 51, 5431-5440.

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Cloned(Commentary)

Cloned (Comment)	Organism
expressed in baculovirus-infected Sf9 cells	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
(E)-4-[3-(5-(adamant-1-yl)-2-(but-1-oxy)-4-(2-methoxyethoxymethoxy)-phenyl)-3-oxoprop-1-en-1-yl]benzoic acid	shows highest inhibition of IKKbeta and highest induction of apoptosis in Jurkat cells	Homo sapiens
(E)-4-[3-(5-(adamant-1-yl)-2-(hexyl-1-oxy)-4-(2-methoxyethoxymethoxy)phenyl)-3-oxoprop-1-en-1-yl]benzoic acid	exhibits improved anti-IKKbeta and growth inhibitory activities and has lost its RAR-dependent transactivation function	Homo sapiens
(E)-4-[3-(5-(adamant-1-yl)-2-ethoxy-4-(2-methoxyethoxymethoxy)phenyl)-3-oxoprop-1-en-1-yl]benzoic acid	-	Homo sapiens
(E)-4-[3-(5-(adamant-1-yl)-4-(2-methoxyethoxymethoxy)-2-(pentyl-1-oxy)phenyl)-3-oxoprop-1-en-1-yl]benzoic acid	-	Homo sapiens
(E)-4-[3-(5-(adamant-1-yl)-4-(2-methoxyethoxymethoxy)-2-(prop-2-en-1-oxy)phenyl)-3-oxoprop-1-en-1-yl]benzoic acid	-	Homo sapiens
(E)-4-[3-(5-(adamant-1-yl)-4-(2-methoxyethoxymethoxy)-2-(prop-2-yn-1-oxy)phenyl)-3-oxoprop-1-en-1-yl]benzoic acid	shows highest inhibition of IKKbeta and highest induction of apoptosis in Jurkat cells	Homo sapiens
(E)-4-[3-(5-(adamant-1-yl)-4-(2-methoxyethoxymethoxy)-2-phenylmethoxy-phenyl)-3-oxoprop-1-en-1-yl]benzoic acid	exhibits improved anti-IKKbeta and growth inhibitory activities and has lost its RAR-dependent transactivation function	Homo sapiens
(E)-4-[3-(5-adamant-1-yl-4-(2-methoxyethoxymethoxy)-2-(prop-1-oxy)-phenyl)-3-oxoprop-1-en-1-yl]benzoic acid	-	Homo sapiens
chalcone	-	Homo sapiens
MX781	0.02 mM inhibit IKKbeta by 65% in the presence of an ATP concentration corresponding to its Km value	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	O14920	-	-

Posttranslational Modification

Posttranslational Modification	Comment	Organism
phosphoprotein	-	Homo sapiens

Source Tissue

Source Tissue	Comment	Organism	Textmining
breast carcinoma cell	-	Homo sapiens	-
JURKAT cell	-	Homo sapiens	-
MDA-MB-468 cell	-	Homo sapiens	-
PC-3 cell	-	Homo sapiens	-
T-47D cell	-	Homo sapiens	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
ATP + IkappaBalpha	-	Homo sapiens	ADP + phosphorylated IkappaBalpha	-	?

Synonyms

Synonyms	Comment	Organism
IKKbeta	-	Homo sapiens

Temperature Optimum [°C]

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

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.007	-	-	Homo sapiens	chalcone

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Release 2023.1 (January 2023)