2H-1,4-Benzoxazine-7-carboxamide, N-cyclopropyl-3,4-dihydro-3-oxo-N-[[4-[(4-pyrimidinylamino)carbonyl]phenyl]methyl]-

UNC6934 (2561494-77-5) is a 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).

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Dilworth et al. (2022), A chemical probe targeting the PWWP domain alters NSD2 nucleolar localization; Nat. Chem. Biol., 18 56