U0126

U0126 (CAS 109511-58-2) is a cell-permeable, non-ATP competitive, selective inhibitor belonging to the class of small molecule kinase inhibitors, functioning as an inhibitor of MEK1 and MEK2 in signal transduction pathways and exhibiting suppression of downstream ERK phosphorylation in various cellular systems. Additionally, it acts as an inhibitor of autophagy and mitophagy processes.

In in vitro experimental settings, U0126 demonstrates effective inhibition of MEK1 and MEK2 with IC50 values of 72 nM and 58 nM, respectively, tested against recombinant kinase assays and cell line models. It can also disrupt the activation of ERK1/2 MAP kinases and block signal propagation within the Raf/MEK/ERK pathway, thereby affecting cell proliferation, differentiation, and survival signals.

In application contexts such as studies on cancer biology, cell signaling, and neurobiology, U0126 is widely used for dissecting the roles of the MAPK/ERK pathway and its contribution to cellular responses to growth factors and stress stimuli. As a research tool, it aids in delineating the contribution of MEK-mediated signaling to disease progression, drug response, and cell fate determination. U0126’s capacity to inhibit autophagy and mitophagy further supports its value in experimental investigation of these degradative processes.