NOTUMib-1 | NOTUM inhibitor, restores Wnt signaling

NOTUM is a carboxylesterase which depalmitoylates Wnt proteins which results in disruption of Wnt signaling¹. 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 activity². NOTUM inhibitors have potential as new therapeutics for degenerative diseaes³.

References/Citations
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., Advance Article
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