Objective: Baicalein had been proved to have anti-cancer activity in vitro and in vivo, including the inhibition of malignant proliferation, migration, adhesion and invasion of many kinds of cancer cells. The special AT-rich sequence binding protein 1(SATB1) is a tissue-specific expression of nuclear matrix-binding protein and is reported to be a breast cancer “gene group organizer”. Previous studies have shown that SATB1 is involved in the growth, metastasis and prognosis of breast cancer. The present study was aimed to investigate whether baicalein inhibits the proliferation and migration of MDA-MB-231 human breast cancer cells through down-regulation of the SATB1 expression. Methods: MDA-MB-231 cells were treated for 24 h, 48 h and 72 h with various concentrations of baicalein(0, 5, 10, 20, 40 and 80 μM) respectively. Then, the proliferation and migration of MDA-MB-231 cells following treatment with baicalein were determined using colorimetric 3-(4, 5-dimethylthiazol-2-yl) 2, 5-diphenyltetrazolium bromide(MTT) and wound healing assays. Thereafter, western blot analysis was performed to detect the changes of SATB1 protein expression in MDA-MB-231 cells. Results: Along with the prolongation of time and increase of drug concentration, inhibitory effect of baicalein on proliferation and migration of MDA-MB-231 cells gradually increased, in a time- and dose- dependent manner(P < 0.05). Meanwhile, after treated with baicalein in different concentrations for 48 h, the level of SATB1 protein expression of MDA-MB-231 cells decreased obviously, in a dose-dependent manner(P < 0.05). Conclusion: Baicalein inhibits breast cancer cell proliferation and suppresses its invasion and metastasis by reducing cell migration possibly by down-regulation of the SATB1 protein expression, indicating that baicalein is a potential therapeutic agent for human breast cancer. Objective: Baicalein had been proved to have anti-cancer activity in vitro and in vivo, including the inhibition of malignant proliferation, migration, adhesion and invasion of many kinds of cancer cells. The special AT-rich sequence binding protein 1 (SATB1) is a tissue-specific expression of nuclear matrix-binding protein and is reported to be a breast cancer “” gene group organizer ". Previous studies have shown that SATB1 is involved in the growth, metastasis and prognosis of breast cancer. The present study was aimed at investigating whether baicalein inhibits the proliferation and migration of MDA-MB-231 human breast cancer cells through down-regulation of the SATB1 expression. Methods: MDA-MB-231 cells were treated for 24 h, 48 h and 72 h with various concentrations of baicalein (0, 5, 10, 20, 40 and 80 μM) respectively. Then, the proliferation and migration of MDA-MB-231 cells following treatment with baicalein were determined using colorimetric 3- (4,5-dimethylthiazol- -yl) 2, 5-d Western blot analysis was performed to detect the changes of SATB1 protein expression in MDA-MB-231 cells. Results: Along with the prolongation of time and increase of drug concentration, inhibitory effect of After, with treated with baicalein in different concentrations for 48 h, the level of SATB1 protein expression of Conclusion: Baicalein inhibits breast cancer cell proliferation and suppresses its invasion and metastasis by reducing cell migration possibly by down-regulation of the SATB1 protein expression, (P <0.05) indicating that baicalein is a potential therapeutic agent for human breast cancer.