UNC0646

UNC0646 is a potent and selective histone methyltransferase G9a inhibitor with an IC₅₀ of 6 nM. UNC0646 is also a potent GLP inhibitor (IC₅₀ <15 nM) and highly selective for G9a/GLP over SETD7, SUV39H2, SETD8 and PRMT3. UNC0646 reduces H3K9me2 levels in MDA-MB-231 cells with an IC₅₀ of 26 nM^[1]. In Vitro:UNC0646 (Compound 6) has high cellular potency and excellent separation of functional potency versus cell toxicity in a variety of cell lines. UNC0646 is highly potent in reducing H3K9me2 levels and has low cell toxicity. UNC0646 reduces H3K9me2 levels with ICW IC₅₀ values of 26 nM, 10 nM, 12 nM, 14 nM, 68 nM, 86 nM and 10 nM in MDA-MB-231, MCF7, PC3, 22RV1, HCT116 wt, HCT 116 p53^-/- and IMR90 cell lines, respectively^[1].