In this study, we showed that 4-cholesten-3-one exerts promising antiproliferative activity and inhibits migration of human MCF-7 and MDA-MB-231 breast cancer cells by (1) reducing lipogenesis and cholesterol biosynthesis (2) increasing the mRNA expression of the ABCG1 and ABCA1 transporters, and by (3) disrupting membrane rafts. This evidence concerns the gene ABCG1 and breast carcinoma.