MEK Inhibitor I is a cell-permeable, pyridine-containing, vinylogous cyanamide that has the ability to act as a selective and potent inhibitor of MEK with little activity towards MKK3 and MKK4. The compound displays significant affinity only towards ATP-bound MEK (i.e. noncompetitive with respect to ATP) and the demonstrated inhibition is noncompetitive with respect to ERK. Compared to U0126 in aqueous solutionsMEK Inhibitor I demonstrates superior potency, solubility, and stability. Additionally shown to protect against phorbol ester-mediated ear edema in mice.
1. Wityak, J., et al. 2004. Bioorg. Med. Chem. Lett. 14: 1483-1486. PMID: 15006386