Drug intelligence / Profile preview

IWP-2

Development stage
Preclinical
Lead developer
UT Southwestern Medical Center
Modality
Small Molecules
Administration
Oral
01

Overview

IWP-2 is a small molecule inhibitor of the Wnt signaling pathway. It specifically targets the enzyme Porcupine (PORCN), a membrane-bound O-acyltransferase (MBOAT) responsible for the palmitoylation of Wnt proteins. This post-translational modification is critical for the secretion and biological activity of Wnt ligands. By blocking Porcupine, IWP-2 prevents the activation of both canonical (β-catenin-dependent) and non-canonical Wnt signaling pathways. In research settings, it is frequently used to investigate the role of Wnt signaling in development, stem cell biology, and various cancers, including multiple myeloma, where it has been shown to reverse resistance to proteasome inhibitors like bortezomib.

Other names
Inhibitor of Wnt Production-2
02

Targets

PORCN (Porcupine protein)CSNK1D (Casein kinase I delta)

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