LGK974，L974-002/010/050

產品信息

Wnt通路調節動物發育過程中的多個重要環節，例如細胞增殖、細胞遷徙及細胞分化。Wnt信號通路調控劑通過自分泌或旁分泌作用與位于細胞膜上的受體相結合，激活細胞內信號通路調節靶基因的表達，對細胞的增殖、分化、遷移、極性化和凋亡起到重要作用

LGK974 is a potent and specificinhibitor of O-acyltransferase Porcupine (Porcn) that acylates Wnt proteins required for their biological activities. The structure of LGK974 was recently published and found not only more potent than the IWP-1, 2, 3 or IWP-4 Porcn inhibitors, but LGK974 is also suitable for in-vivo studies and is currently in Phase I clinical trials to treat cancers.

Purity:
Greater than 99% as determined by LC/MSanalysis.

Biological Activity:
Biological activity has been determined. In a co-culture assay measuring the activation of the TCF reporter gene by Wnt3a-secreting cells, this compound gives IC50 of 0.2to 0.6nM. Pan and colleagues reported antitumor activity of LGK974 in xenograft models of human head and neck as well as pancreatic tumors when dosed at 1 to 10 mg/kg orally.

重慶市華雅干細胞技術有限公司