UNC6934
NSD2 inhibitor / 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).
Biochemicals & reagents
2561494-77-5
Dilworth et al. (2022), A chemical probe targeting the PWWP domain alters NSD2 nucleolar localization; Nat. Chem. Biol., 18 56
-20°C
TARGET: Protein methyltransferase -- PATHWAY: Chromatin; Posttranslational modification; Transcription; Bcl; AKT; ERK -- RESEARCH AREA: Epigenetics -- DISEASE AREA: Cancer