Collectively, this study revealed that CuB inhibited TGF-β1-induced EMT in NSCLC cells and Gefitinib resisitant NSCLC cells through regulating ROS and PI3K/Akt/mTOR pathways, which might be a promising therapeutic agent for NSCLC and EGFR-TKIs resistant NSCLC. The gene discussed is TGFB1; the disease is non-small cell lung carcinoma.