Catalog Number: 4343
Chemical Name: 2-Cyclohexyl-6-methoxy-N-[1-(1-methylethyl)-4-piperidinyl]-7-[3-(1-pyrrolidinyl)propoxy]-4-quinazolinamine
Biological Activity
Selective inhibitor of G9a and GLP histone lysine methyltransferases (IC50 values are < 15 nM and 19 nM for G9a and GLP respectively, and > 10000 nM for a range of other histone methyltransferases). Potently inhibits dimethylation of H3K9 in MCF-7 cells (IC50 = 70 nM). Cell permeable.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 100 mM in DMSO and to 100 mM in ethanol and to 100 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 0638 probe summary on the SGC website.
Background References
  1. A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells.
    Vedadi et al.
    Nat.Chem.Biol., 2011;7:566
  2. Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines.
    Liu et al.
    J.Med.Chem., 2011;54:6139
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