UNC0638

Description: UNC0638 is a selective and cell-permeable inhibitor of G9a histone methyltransferase and GLP with IC50 of< 15 nM and 19 nM, respectively, it shows selectivity over a wide range of epigenetic and non-epigenetic targets. UNC0638 showed balanced physicochemical properties and potency aiding cell penetration in vitro, had high potency in cellular assays. It was much less toxic than BIX01294 to cells. In MDA-MB-231 cells, in a concentration-dependent manner, exposure to UNC0638 for 48 h reduced H3K9me2 levels with an IC50 value of 81 +/- 9 nM (n= 3), which showed considerably higher potency than BIX01294 (IC50= 500 +/- 43 nM (n= 3)). In reducing H3K9me2 levels, UNC0638 was of greater maximum effect than BIX01294. This effect is close, but not equal, to the effect on the double knockdown of G9a and GLP via shRNA.

References: Nat Chem Biol. 2011 Jul 10; 7(8):566-74.