Brief Description

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].
References on Kartogenin:
[1]. Johnson K, et al. A stem cell-based approach to cartilage repair. Science. 2012 May 11;336(6082):717-21.
[2]. Wang J, et al. A heterocyclic molecule kartogenin induces collagen synthesis of human dermal fibroblasts by activating the smad4/smad5 pathway. Biochem Biophys Res Commun. 2014 Jul 18;450(1):568-74.

Solubility

DMSO 59 mg/ml

Melting point

Boiling point

Density

Formula Weight:

Flash point

Storage conditions

Store at -20°C 2 years

Appearance:

White to off-white solid