scavengers) and calpeptin (calpain inhibitors) significantly attenuated Rk1-induced apoptosis. Moreover, Rk1 significantly inhibited the growth of SK-MES-1 xenograft tumors with low toxic side effects. In summary, this study for the first time demonstrated that Rk1 had significant antitumor effects against lung squamous cell carcinoma and great potential to serve as a novel anticancer agent.