Potent and selective inhibitor of the homologous protein lysine methyltransferases, G9a and GLP (IC50
values are 6 nM and 15 nM for G9a and GLP, respectively). Potently blocks G9a/GLP methyltransferase activity in cells (IC50
= 10 nM in MCF7 cells); exhibits low cellular toxicity (EC50
= 4.7 μ
M in MCF7 cells). Selective for G9a/GLP over a range of other protein lysine methyltransferases and protein arginine methyltransferases.
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All Tocris products are intended for laboratory research use only.
Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines.
Liu et al.