Catalog Number: 5155
Chemical Name: N-[4-[(2-Amino-6-methyl-4-pyrimidinyl)amino]phenyl]-4-(4-quinolinylamino)benzamide
Biological Activity
DNA methyltransferase inhibitor. Inhibits the mammalian DNA methyltransferases DNMT3B, DNMT3A and DNMT1 (IC50 values are 7.5, 8 and 12.5 μM with Poly(dl-dC) as the substrate). Reactivates silenced tumor suppressor genes by reducing CpG island hypermethylation.
Technical Data
  • M.Wt:
    461.52
  • Formula:
    C27H23N7O
  • Solubility:
    Soluble to 50 mM in DMSO
  • Purity:
    >99%
  • Storage:
    Store at -20°C
  • CAS No:
    1020149-73-8
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.
Background References
  1. A new class of quinoline-based DNA hypomethylating agents reactivates tumor suppressor genes by blocking DNA methyltransferase 1 activity and inducing its degradation.
    Datta et al.
    Cancer Res., 2009;69:4277
  2. Synthetic approaches to DNMT inhibitor SGI-1027 and effects on the U937 leukemia cell line.
    Garc?a-Dom?nguez et al.
    Bioorg.Med.Chem.Lett., 2013;23:1631

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