Embelin, a small molecule XIAP (X-linked inhibitor of apoptosis protein) inhibitor, can inhibit the expression and activation of XIAP, thereby removing the antiapoptotic ability of XIAP and resulting in apoptosis process smoothly. This study is attempt to explore the mechanism of the inhibition to hepatocarcinoma cell Bel-7404 growth by Embelin. After treated with different-concentration of Embelin, the morphological change, formation of apoptotic bodies, cells viability, cell apoptosis and the apoptosis-related protein expression in Bel-7404 cells were assessed by fluorescence microscope, Hochest33342 staining, MTT assay, Annexin Ⅴ/PI flow cytometry and Western blotting et al. The results indicated that Embelin remarkably inhibited human hepatocarcinoma cell Bel-7404 growth. Further experiments found that the mechanism of tumor cell growth inhibition by Embelin was due to the cell apoptosis with the activation of caspase apoptotic pathway and blockage of NF-κB signal pathway. The studies laid a base on the further treatment of human hepatoma carcinoma by using Embelin.