Catalog Number: 5132
Chemical Name: 2-(4,4-Difluoro-1-piperidinyl)-6-methoxy-N-[1-(1-methylethyl)-4-piperidinyl]-7-[3-(1-pyrrolidinyl)propoxy]-4-quinazolinamine
Biological Activity
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.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 100 mM in DMSO and to 50 mM in 1eq. HCl
  • Purity:
  • Storage:
    Store at +4°C
  • CAS No:
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.
Additional Information
Licensing Caveats:
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.
Background References
  1. Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP.
    Liu et al.
    J.Med.Chem., 2013;56:8931
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