Description
Kartogenin potently induces differentiation of human mesenchymal stem cells into chondrocytes with an EC
50 value of 100 nM. Kartogenin induces chondrogenesis by binding the actin-
binding protein, filamin A, which disrupts its interaction with the transcription factor core-
binding factor β subunit (CBFβ). When dissociated from filamin A, CBFβ translocates to the nucleus and forms a transcriptional complex with the runt-
related transcription factor RUNX1, which enables chondrocyte differentiation. Kartogenin has been shown to promote cartilage repair in a mouse model of osteoarthritis and to protect against cytokine-
induced damage in osteoarthritic bovine articular chondrocytes
in vitro.
Uses
Kartogenin is a potent, selective, and non-cytotoxic downstream RUNX1 and RUNX2 modulator. Kartogenin causes mesenchymal stem cells found in joints to differentiate into chondrocyte cells that can build cartilage where it has been destroyed.
Biochem/physiol Actions
Kartogenin induces the selective differentiation of multipotent mesenchymal stem cells (MSCs) into chondrocytes. Kartogenin binds to filamin A, and disrupts the specific interaction between filamin A and CBFβ (core-binding factor β subunit). Apparently, kartogenin induces chondrogenesis by regulating the nuclear localization of CBFβ.
