Here, in vitro and in vivo experimental data showed that baicalin prevents cell cycle progress by blocking cell transition from G1 phase to S phase (arresting cell cycle at G1-phase), inhibits EMT of CRC cells by inhibiting TGFβ/Smads pathway, and attenuates CRC cell stemness by decreasing the levels of cancer stem cell markers; and simultaneously, baicalin also initiates and induces CRC cell apoptosis by activating Caspase-dependent signal pathways. The gene discussed is TGFB1; the disease is colorectal carcinoma.