PFI-653 a chemical probe to study the role of Vanin-1 in inflammatory diseases of the digestive tract
Vanin-1 (VNN-1) is a member of the nitrilase superfamily. Its primary function is the recycling of pantothenic acid (vitamin B5), an important precursor in the biosynthesis of CoenzymeA. VNN-1 has been reported to control inflammatory responses in many tissues showing a significant increase in expression in biopsies of inflammatory bowel disease (IBD) patients at sites of inflammation. IBD is a chronic inflammatory syndrome of the digestive tract and patients suffer from persistent diarrhea, abdominal pain and other symptoms.
PFI-653 is a competitive inhibitor of VNN-1 with an IC50 of 6.85 nM (hVanin1) and no significant off-targets in protease, kinase, CEREP and PDE panels.
PFI-653 and its negative control are very well suited to study the role of VNN-1 in inflammatory and other diseases.
Crystal structure of PFI-653 (purple)bound to vanin-1 at 2.13 Å resolution (PDB 7SLV).
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For more information about the chemical probe MS023 visit the SGC website.
Chemical probe PFI-653 Negative control PFI-653-N
The chemical probe PFI-653 and the negative control compound can be ordered here.