bay1143269

BAY1143269 is an orally bioavailable, potent, and selective small molecule inhibitor of mitogen‐activated protein kinase interacting serine/threonine‐protein kinase 1 (MKNK1). It was developed as an antineoplastic agent with the primary mechanism of action being inhibition of MKNK1, which prevents its activation and downstream phosphorylation events. This leads to suppression of eukaryotic translation initiation factor 4E (eIF4E) phosphorylation and reduced expression of oncogenic proteins involved in cell cycle progression, epithelial-mesenchymal transition, survival pathways, and angiogenesis. Preclinical studies demonstrated anti-cancer and anti-angiogenic activity in glioblastoma models. Clinical development included phase I trials for advanced solid tumors; however, further development has been discontinued[2][3][5][6].

Other names

BAY1143269BAY-1143269BAY 1143269