Taken together, our data confirmed that copper chelation therapy significantly reduces EMT by downregulating TGF-β/pSMAD2, and TGF-β/PI3K/p-AKT, TGF-β/RAS/RAF/MEK/ERK, and TGF-β/WNT/β-catenin pathways in cancer cells. This evidence concerns the gene TGFB1 and cancer.