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The synthetic triterpenoid 1-[2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oyl]imidazole blocks nuclear factor- B activation through direct inhibition of I B kinase
Molecular Cancer Therapeutics
The synthetic triterpenoid 1-[2-cyano-3,12-dioxooleana-1, 9(11)-dien-28-oyl]imidazole (CDDO-Im) is a multifunctional agent with potent anti-inflammatory, antiproliferative, cytoprotective, and apoptotic activities, whose molecular targets are unknown. Using both cell-free and cellular assays, we show that CDDO-Im is a direct inhibitor of IKB kinase (IKK) B and that it thereby inhibits binding of nuclear factor-KB to DNA and subsequent transcriptional activation. Pretreatment of cells withdoi:10.1158/1535-7163.mct-06-0444 pmid:17148759 fatcat:jcadhslfbfe2doamfc2vqh2bgi