Kartogenin, 2-[([1,1'-Biphenyl]-4-ylaMino)carbonyl]benzoic Acid;2-[(Biphenyl-4-yl)carbaMoyl]benzoic Acid;4'-Phenylphthalanilic Acid;Kartogenin;KGN;2-([1,1'-biphenyl]-4-ylcarbaMoyl)benzoic acid;4′-Phenyl-phthalan 4727-31-5
Kartogenin(KGN) is a small molecule stimulator of chondrogenesis; promotes chondrocyte differentiation(EC50=100 nM) and binds to filamin A.
IC50 value: 100 nM(EC50, promotes chondrocyte differentiation) [1]
Target: Chondrogenesis stimulator
Kartogenin is a small molecule kartogenin, which promotes chondrocyte differentiation (median effective concentration = 100 nM), shows chondroprotective effects in vitro, and is efficacious in two OA animal models. Kartogenin binds filamin A, disrupts its interaction with the transcription factor core-binding factor β subunit (CBFβ), and induces chondrogenesis by regulating the CBFβ-RUNX1 transcriptional program [1]. KGN stimulated type-I collagen synthesis of fibroblasts at the mRNA and protein levels in a time-dependent manner, but KGN did not induce expression of α-skeletal muscle actin (α-sma) or matrix metallopeptidase1 (MMP1), MMP9 in vitro [2]. KGN promoted the type-I collagen synthesis of dermal fibroblasts in vitro and in the dermis of mice through activation of the smad4/smad5 pathway.
in vivo: KGN also increased type-I collagen synthesis in the dermis of BALB/C mice [2].
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