NOTUM is a carboxylesterase which depalmitoylates Wnt proteins which results in disruption of Wnt signaling.1?NOTUMib-1 inhibits the carboxylesterase activity of NOTUM, IC50=0.085 μM, and restores Wnt signaling. An important new tool for use in cellular disease models in which overactivity of NOTUM suppresses Wnt activity.2?NOTUM inhibitors have potential as new therapeutics for degenerative diseases.3
NOTUMib-1 is a NOTUM inhibitor. NOTUM inhibitors have potentials as new therapeutics for degenerative diseases.
1) Zhang?et al.?(2016),?Methods for Studying Wnt Protein Modifications/Inactivations by Extracellular Enzymes Tiki and Notum; Methods Mol. Biol.,?1481?29
2) Atkinson?et al.?(2019),?Discovery of 2-phenoxyacetamides as inhibitors of the Wnt-depalmitoleating enzyme NOTUM from an X-ray fragment screen; Med. Chem. Commun.?10?1361
3) Suciu?et al.?(2018),?Selective Irreversible Inhibitors of the Wnt-Deacylating Enzyme NOTUM Developed by Activity-Based Protein Profiling; ACS Med. Chem. Lett.,?9?563
