UNC0642,G9a/GLPHMTaseInhibitor

UNC0642 is a novel highly potent, selective and cell permeable inhibitor of the homologous protein lysine methyltransferases, G9a and GLP, with IC₅₀ < 2.5 nM. It has selectivity > 1000-fold over 13 other HMTs and selected representatives of kinases, ion channels, 7TMs, and other epigenetic proteins. UNC0642 reduces H3K9 dimethylation levels in MDA-MB-231 cells (IC₅₀~110 nM). It has improved PK properties relative to UNC0638 and displayed modest brain penetration in vivo.

How to Use:

• In vitro:  UNC0642 was used at 0.5 µM in vitro and cellular assays. 
• In vivo: UNC0642 was dosed to mice by intraperitoneal injection (IP) at 5 mg/kg once per day.

Reference:

• 1. Liu F, et al. Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP. (2013) J Med Chem. 56(21):8931-42.