Ginsenoside Rp1 (G-Rp1) is a novel ginseng saponin with a chemopreventive action. In this study, we examined the anti-metastatic activities of G-Rp1 using relevant in vitro assays and in vivo metastasis models. Using a U937 cell-cell adhesion assay, we found that exogenously added G-Rp1 down-regulates beta1-integrin (CD29) activation at concentrations between 10 to 40 microM and suppresses the in vitro tube formation of human umbilical vein endothelial cells (HUVECs). Furthermore, this compound directly blocked cell viability of cancer cells such as A549 and HCT15 cells. In agreement with in vitro findings, G-Rp1 strongly inhibited the metastatic lung transfer of B16-F10 melanoma cells, which have a high surface level of beta1-integrins, without altering body weight. Therefore, these results suggest that G-Rp1 may act as an anti-cancer agent by strongly inhibiting cell viability and metastatic processes, presumably by inhibiting the adhesion of tumor cells and vessel formation.