UNC0642

UNC0642 is a potent, selective and cell-permeable inhibitor of G9a (EHMT2) and GLP (EHMT1) histone lysine methyltransferases. UNC0642 exhibits an in vitro IC₅₀ <15 nM with selectivity > 100-fold over 13 other HMTs and selected representatives of kinases, ion channels, 7TMs, and other epigenetic proteins. In cells, UNC0642 results in a potent reduction of H3K9me2 in MDA MB231 cells with IC₅₀ = 106 nM.