IWP-2,Porcupine(Wnt)Inhibitor

IWP-2 is a potent and highly selective Wnt signaling antagonist with an IC₅₀ ~ 27 nM in the L-Wnt-STF cellular assay. It prevents palmitoylation of Wnt proteins by Porcupine (a membrane-bound O-acyltransferase), thereby blocking Wnt protein secretion and activity. It blocks Wnt-dependent phosphorylation of Lrp6 receptor and Dvl2, and β-catenin accumulation. IWP-2 is a useful chemical probe in both regenerative medicine and anticancer efforts.

How to Use:

• In vitro: IWP-2 was used at 1-2 µM in vitro and in cellular assays.
• In vivo: n/a

Reference: 

• 1. Chen B, et al. Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. (2009) Nat Chem Biol. 5(2):100-7.
• 2. ten Berge D, et al. Embryonic stem cells require Wnt proteins to prevent differentiation to epiblast stem cells. (2011) Nat Cell Biol. 13(9):1070-5.
• 3. Lian X, et al. Robust cardiomyocyte differentiation from human pluripotent stem cells via temporal modulation of canonical Wnt signaling. (2012) Proc Natl Acad Sci USA. 109(27):E1848-57.      

Products are for research use only. Not for human use.