UNC0642 (UNC 0642) is a potent and selective G9a and GLP histone lysine methyltransferase inhibitor with IC50 of <2.5 nM.
UNC0642 displays >2,000-fold selectivity for G9a and GLP over PRC2-EZH2 and >20,000-fold selectivity over other methyltransferases.
UNC0642 reduces H3K9 dimethylation levels with IC50 of <150 nM in U2OS, PC3, and PANC-1 cells, exhibits excellent potency (IC50 = 40 nM) in PANC-1 cells.
UNC0642 reduces clonogenicity in PANC-1 cells in a concentration-dependent manner while it had no effect on clonogenicity in MDA-MB-231 cells.
