Catalog Number: 5590
Chemical Name: 4-[4-[(Dimethylamino)methyl]-2,5-dimethoxyphenyl]-2-methyl-1,2-dihydro-2,7-naphthyridin-1-one
Biological Activity
Potent and selective BRD9 and BRD7 inhibitor (Kd values are 14 and 239 nM, respectively). Exhibits selectivity for BRD9/7 over 48 other bromodomains, 324 kinases and 55 GPCRs. Inhibits proliferation of AML cell lines in vitro and reduces AML tumor xenograft growth in vivo. Cell permeable and orally active.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 20 mM in DMSO and to 10 mM in 1eq. HCl with gentle warming
  • Purity:
  • Storage:
    Store at -20°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 BI 9564 probe summary on the SGC website.
Background References
  1. Structure-based design of an in vivo active selective BRD9 inhibitor
    Martin et al.
    J.Med.Chem., 2016;59:4462
  2. An Advanced Tool To Interrogate BRD9.
    Karim and Schönbrunn
    J.Med.Chem., 2016;59:4459
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