UNC0646,G9a/GLPHMTaseInhibitor

UNC0646 is a novel potent, selective and cell permeable inhibitor of the homologous protein lysine methyltransferases, G9a and GLP, with IC₅₀ ~6 nM and 15 nM for G9a and GLP, respectively. It potently inhibits G9a/GLP methyltransferase activity in cells (IC₅₀ ~10 nM in MCF7 cells), and exhibits low toxicity. It is highly selective for G9a/GLP over several other protein lysine and arginine methyltransferases. UNC0646 did not affect G9a co-activator function but selectively decreased G9a co-repressor function for endogenous target genes. 

How to Use:

• In vitro:  UNC0646 was used at 2 µM in vitro and cellular assays. 
• In vivo: n/a

Reference:

• 1. Liu F, et al. Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines. (2011) J Med Chem. 54(17):6139-50.
• 2. Bittencourt D, et al. G9a functions as a molecular scaffold for assembly of transcriptional coactivators on a subset of glucocorticoid receptor target genes. (2012) Proc Natl Acad Sci USA. 109(48):19673-8.