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Bioorg Med Chem Lett. 1998 Oct 20;8(20):2839-44.

MEK inhibitors: the chemistry and biological activity of U0126, its analogs, and cyclization products.

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DuPont Pharmaceuticals Company, Chemical and Physical Sciences Department, Wilmington, DE 19880, USA.


In search of antiinflammatory drugs with a new mechanism of action, U0126 was found to functionally antagonize AP-1 transcriptional activity via noncompetitive inhibition of the dual specificity kinase MEK with an IC50 of 0.07 microM for MEK 1 and 0.06 microM for MEK 2. U0126 can undergo isomerization and cyclization reactions to form a variety of products, both chemically and in vivo, all of which exhibit less affinity for MEK and lower inhibition of AP-1 activity than parent, U0126.

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