The aim of the present study was to investigate the effects of baicalein on the protein expression of SATB1 in the MDA-MB-231 human breast cancer cell line. MDA-MB-231 cells were treated with various concentrations of baicalein (0, 10, 20, 40 µM). Following treatment, a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide assay and wound healing assay were used to detect the changes in cell proliferation and migration. In addition, western blot analysis was performed to detect the changes in the protein expression levels of SATB1 in the MDA-MB-231 cell line. With the prolongation of administration time and the increase in drug concentration, the inhibitory effect of baicalein on the proliferation and migration of MDA-MB-231 cells gradually increased in a time- and dose-dependent manner (P<0.05). In addition, baicalein was shown to markedly decrease the protein expression levels of SATB1 in the MDA-MB-231 cells. With increasing drug concentrations, the protein expression levels of SATB1 decreased gradually (P<0.05). Therefore, baicalein was demonstrated to inhibit the proliferation of MDA-MB-231 cells and downregulate the protein expression of SATB1, indicating that baicalein can significantly inhibit the proliferation, migration and invasiveness of MDA-MB-231 cells by downregulating the expression of SATB1.