Literature summary for 2.7.11.10 extracted from

Yan, S.S.; Li, Y.; Wang, Y.; Shen, S.S.; Gu, Y.; Wang, H.B.; Qin, G.W.; Yu, Q.
17-Acetoxyjolkinolide B irreversibly inhibits IkappaB kinase and induces apoptosis of tumor cells (2008), Mol. Cancer Ther., 7, 1523-1532.

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Application

Application	Comment	Organism
medicine	17-acetoxyjolkinolide B is a novel type NF-kappaB pathway inhibitor. Its unique interaction mechanism with IKK may render it a strong apoptosis inducer of tumor cells and a novel type anticancer drug candidate	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
17-acetoxyjolkinolide B	17-AJB is isolated from a traditional Chinese medicinal herb Euphorbia fischeriana Steud. 17-AJB interacts with IKK directly and keeps IKK in its phosphorylated form irreversibly, inactivating its kinase activity, leading to its failure to activate NF-kappaB. The effect of 17-AJB on IKK is specific. It has no effect on other kinases such as p38, p44/42, and JNK. 17-AJB induces apoptosis in tumor cells	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	O14920	-	-

Posttranslational Modification

Posttranslational Modification	Comment	Organism
phosphoprotein	activation of IKKbeta requires phosphorylation on Ser177/Ser181 of its active loop. 17-acetoxyjolkinolide B increases the phosphorylation of IKKbeta	Homo sapiens

Source Tissue

Source Tissue	Comment	Organism	Textmining
Hep-G2 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
37	-	assay at	Homo sapiens

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.0003	-	-	Homo sapiens	17-acetoxyjolkinolide B

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Release 2023.1 (January 2023)