A-366

  • Chemical Properties
CAS No. 1527503-11-2 Cat. No. BCP17827
Name A-366
Synonyms A 366;A366;
Formula C19H27N3O2 M. Wt 329.44
  • Biological Activity
Description A-366 is a potent inhibitor of G9a/GLP with IC50 3 nM and > 100-fold selectivity over other methyltransferases and other non-epigenetic targets. A-366 has been shown to inhibit H3K9 methylation in cells with an IC50 of 100 nM and exhibits minimal cellular toxicity compared with previous quinazoline-based probes. A-366 selectively inhibits G9a and the closely related GLP (EHMT1), but not other histone methyltransferases. A-366 has significantly less cytotoxic effects on the growth of tumor cell lines compared to other known G9a/GLP small molecule inhibitors despite equivalent cellular activity on methylation of H3K9me2.
Pathways Epigenetics 
Targets Histone Methyltransferase 

Structure

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