Reprogramming cell fates towards pluripotent stem cells and other cell types has revolutionized our understanding of cellular plasticity.During the last decade,transcription factors and microRNAs have become powerful reprogramming factors for modulating ceil fates.Recently,many efforts are focused on reprogramming cell fates by non-viral and non-integrating chemical approaches.Small molecules not only are useful in generating desired cell types in vitro for various applications,such as disease modeling and cellbased transplantation,but also hold great promise to be further developed as drugs to stimulate patients’ endogenous cells to repair and regenerate in vivo.Here we will focus on chemical approaches for generating induced pluripotent stem cells,neurons,cardiomyocytes,hepatocytes and pancreatic β cells.Significantly,the rapid and exciting advances in cellular reprogramming by small molecules will help us to achieve the long-term goal of curing devastating diseases,injuries,cancers and aging.