R2-8018

R2-8018 is a selective small molecule antagonist of the M3 muscarinic acetylcholine receptor (M3R), developed by researchers at Peking University. It is primarily utilized as a research tool to investigate the role of M3R signaling in oncogenesis, particularly in non-small cell lung cancer (NSCLC). R2-8018 works by inhibiting M3R-mediated transactivation of the epidermal growth factor receptor (EGFR), a process that involves the recruitment of c-Src and beta-arrestin-1. By blocking this pathway, R2-8018 suppresses downstream PI3K/AKT and MEK/ERK signaling, leading to inhibited cell proliferation, migration, and cell cycle progression in NSCLC models.