U0126

U-0126 is a novel, potent and selective MEK inhibitor (MEK1; IC50=72nM, MEK2; IC50=58nM). Inhibits AP-1 transcription activity. Blocks the production of inflammatory cytokines and matrix metalloproteinases. Binding of extracellular growth factors to cell surface receptors often results in activation of the mitogen-activated protein kinase (MAPK). MAPK is regulated by MAPK kinase, also called MEK. Deprivation of growth factors during cell culture or intracellular MEK inhibition leads to inhibition of proliferation and apoptotic cell death. N Blank et al. (2002) have shown that U0126, a common used MEK inhibitor and compound that itself has no intrinsic fluorescence in vitro but develops an intensive fluorescence during cell culture which can be observed in all fluorescence channels with predominance in the FL1 channel (525nm).

1. Duncia J.V., et a.l (1998) Bioorg. Med. Chem. Lett. 8(20): 2839-44. 2. Favata M.F., et al. (1998) J. Biol. Chem. 273(29): 18623-32. 3. Davies S.P., et al. (2000) Biochem. J. 351(Pt1): 95-105. 4. Namura S., et al. (2001) Proc. Natl. Acad. Sci. U.S.A. 98(20): 11569-74.