Potent and selective G9a and GLP histone lysine methyltransferase inhibitor (IC50
< 2.5 nM). Exhibits >2,000-fold selectivity for G9a and GLP over PRC2-EZH2 and >20,000-fold selectivity over other methyltransferases. Reduces H3K9 dimethylation levels in MDA-MB-231 cells (IC50
= 110 nM). Displays modest brain penetration in vivo
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the UNC 0642 probe summary
on the SGC website.
Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP.
Liu et al.