MR837 is an Inhibitor of NSD2-PWWP1
NSD2 (nuclear receptor-binding SET domain-containing 2) is a protein lysine methyltransferase. It belongs to the NSD family, which also includes NSD1 and NSD3, and that predominantly mono- and dimethylates lysine 36 of histone 3 (H3K36). NSD2 is an oncoprotein that is aberrantly expressed, amplified, or somatically mutated in multiple...
BI-9321, a First-in-Class Chemical Probe, is a NSD3-PWWP1 Inhibitor
Post-translational modification of histones by histone-modifying enzymes represents a key element of epigenetic regulation. Epigenetic reader domains are structurally diverse. They include bromodomains, PHD domains, methyl-lysine- and/or methyl-arginine-binding domains, frequently co-locating within the same proteins. By interfering with the function of specific domains, selective chemical probes represent powerful tools...