U0126

U0126 is a potent and selective small molecule inhibitor of mitogen-activated protein kinase kinases MEK1 and MEK2. It acts by noncompetitively inhibiting the kinase activity of MEK1/2, thereby preventing activation of downstream extracellular signal-regulated kinases ERK1/2 in the MAPK/ERK signaling pathway. This pathway regulates diverse cellular processes including proliferation, differentiation, survival, autophagy and apoptosis. U0126 has been widely used as a research tool to study these pathways in contexts such as cancer biology (notably inhibiting anchorage-independent growth in certain breast cancer cell lines), ischemia models and oxidative stress. It is not approved for clinical use but is available commercially for preclinical research purposes. The compound shows little effect on other kinases such as PKC or Raf and has demonstrated brain penetration in some studies.

Other names

1,4-Diamino-2,3-dicyano-1,4-bis(2-aminophenylmercapto)butadiene1,4-Diamino-2,3-dicyano-1,4-bis(2-aminophenylthio)butadiene