IWP-2 is an inactivator of Porcn function, and inhibitor of Wnt production. The Wnt/b-catenin (′canonical′) pathway maintains transcriptional programs that enable stem cells to remain multipotent. Hyperactivation of the Wnt/b-catenin pathway leads to the disease stage. IWP-2 inhibits Wnt production. It appears that IWP-2 inactivates Porcn function either by modulating the function of a Porcn regulator or by directly inhibiting the Porcn active site. Porcn is a member of the membrane-bound O-acyltransferase (MBOAT) family, which adds a palmitoyl group to Wnt proteins that is essential to their signaling ability and is required for Wnt secretion. IWP-2 is useful in both regenerative medicine and anticancer efforts. IWP-2 has been used to suppress embryonic stem cell self-renewal. |