Chemical biology has been attracting a lot of attention because of the key roles of chemical methods and techniques in helping to decipher and manipulate biological systems.Although chemical biology encompasses a broad field,this review will focus on chemical biology aimed at using exogenous chemical probes to interrogate,modify and manipulate biological processes,at the cellular and organismal levels,in a highly controlled and dynamic manner.In this area,many advances have been achieved for cancer biology and therapeutics,from target identification and validation based on active anticancer compounds (forward approaches) to discoveries ofanticancer molecules based on some important targets including protein-protein interaction (reverse approaches).Herein we attempt to summarize some recent progresses mainly from China through applying chemical biology approaches to explore molecular mechanisms of carcinogenesis.Additionally,we also outline several new strategies for chemistry to probe cellular activitiessuch as proximity-dependent labeling methods for identifying protein-protein interactions,genetically encoded sensors,and light activating or repressing gene expression system.