To examine the suitability of hGC33-SFB-NP for targeted HCC therapy, we tested the model conjugates for their ability to bind to human glypican-3 on HCC cells in vitro; to inhibit glypican-3-positive HCC cell proliferation, migration, and Wnt/β-catenin signal transduction; and inhibit HCC that overexpress glypican-3 in vivo. This evidence concerns the gene GPC3 and hepatocellular carcinoma.