White solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A cell-permeable pyridine-containing vinylogous cyanamide compound that acts as a potent and selective inhibitor of MEK (IC50 = 12 nM) with little activity towards MKK3 and MKK4 (IC50 > 1 µM). The inhibition is noncompetitive with respect to ERK and the compound displays significant affinity only towards ATP-bound MEK (i.e. uncompetitive with respect to ATP). Exhibits superior potency, solubility, and stability compared to U0126 (Cat. No. 662005) in aqueous solutions. Shown to protect against phorbol ester-mediated ear edema in mice (ED50 of 5 mg/kg, ip.). Purity: ≥ 95% by HPLC (sum of two isomers). Ref.: Wityak, J., et al. 2004. Bioorg. Med. Chem. Lett. 14, 1483. |
