These files are supporting data for Wang Tianyi's Ph.D. thesis, entitled "Targeting ubiquitin-proteasome system for cancer therapy". In this thesis, nanoparticles or prodrugs are developed for ubiquitin-proteasome system-based therapeutic strategies. The data include chemical synthesis of different chemical tools, characterization of the drugs or materials, cellular studies about how these systems influence intracellular pathways, and in vivo studies about how these platforms perform in tumor-bearing mouse models.