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Osteoarthritis (OA) is predicted to be the fourth leading cause of disability in the world by the year 2020. OA results in damage to cartilage tissue and underlying subchondral bone. Current therapeutic options for osteoarthritis (OA) are limited due to the unique nature of cartilage tissue. Alternatively, mesenchymal stem cells (MSCs) have been utilized for cartilage repair, but the formation of an intact neocartilage similar to hyaline cartilage is still a challenge. Kartogenin (KGN), a small heterocyclic, drug-like compound was discovered in the year 2012. KGN was found to induce chondrogenesis of MSCs and protect chondrocytes against OA. At the molecular level, KGN dissociates Filamin A from CBFβ that translocates into the nucleus and interacts with RUNX1 to transcribe genes involved in the chondrogenesis of MSCs. KGN maintains the balance between anabolism and catabolism of cartilage by providing protection against cytokine-induced cartilage damage. KGN also prevents apoptosis of MSCs and chondrocytes during stress conditions that mimic OA in vitro. Moreover, KGN repaired the damaged cartilage in chemicallyand surgicallyinduced animal models of OA. KGN treatment in mouse and rabbit models of OA improved as assessed by the gross morphology, histological features, MRI, micro-CT and serum markers of OA. Here we present a brief review of KGN in terms of cartilage repair both in vitro and in vivo. To the best of our knowledge, this is a first review that discusses the potential of KGN for cartilage repair.

Kartogenin Induced Chondrogenesis of Stem Cells and Cartilage Repair