As a degenerative disease caused by multiple factors, osteoarthritis is characterized by articular cartilage degeneration and reactive hyperplasia of joint edge and the subchondral bone. Recently, kartogenin (KGN) was identified to promote chondrocyte differentiation. KGN can block interleukin 1β(IL-1β)-caused loss of extracellular matrix and proteoglycan. Transforming growth factor β1(TGF-β1), bone morphogenetic protein 7(BMP-7), and KGN together can synergistically promote the expression of lubricin in chondrocytes. KGN can also induce cartilage-like tissue formation in tendon-bone junction. In addition, chitosan (CHI)-KGN nanoparticles and CHI-KGN microspheres can more effectively induce chondrogenic differentiation than unconjugated KGN. Here in this paper we summarized the roles of KGN in regulating the cartilage regeneration.