UNC6934

Potent (IC50 = 104 nM) and selective inhibitor of protein lysine methyltransferase nuclear receptor-binding SET domain-containing 2 (NSD2) . It potently binds to the PWWP1 domain antagonizing interaction with nucleosomal H3K36me2. UNC6934 is selective against 14 other human PWWP domains and 33 methyltransferases. Active in a nanoBRET PPI assay in U2OS cells (IC50 = 1.23 µM) .