tcsc2095 IWP L6

IWP L6 is a Porcn inhibitor with EC50 of 0.5 nM.

IC50 Value: 0.5 nM(EC50) [1]

Target: Porcupine

in vitro: IWP-L6 effectively suppressed the phosphorylation of dishevelled 2 (Dvl2) in HEK293 cells, a biochemical event associated with many Wnt-dependent cellular responses. IWP-L6 inhibits Wnt mediated branching morphogenesis in cultured embryonic kidneys [1].

in vivo: IWP-L6 is stable in human plasma over 24 h, it was rapidly metabolized in rat plasma (t1/2 = 190 min), murine plasma (t1/2 = 2 min), and the murine liver S9 fractions (t1/2 = 26 min). The major metabolites are the amide cleavage products. Similar species-dependent metabolitic profiles due to the involvement of carboxylesterase (CES) have been reported with other drug candidates. Despite its modest metabolic stability in mouse-derived plasma, IWP-L6 was highly active in zebrafish. IWP-L6 exhibited more potent activity [1].