Kartogenin potently induces differentiation of human mesenchymal stem cells into chondrocytes with an EC50 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.
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.
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.
Kartogenin (10 μM in 4 μL of saline; i.a. on days 7 and 21) promotes cartilag erepair in collagenase VII-induced OA models in mice[1].
[1] KRISTEN JOHNSON. A Stem Cell–Based Approach to Cartilage Repair[J]. Science, 2012, 336 6082. DOI:
10.1126/science.1215157
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