Catalog Number: 5173
Chemical Name: (E)-4-[2-(2-Amino-4-hydroxy-5-methylphenyl)diazenyl]-N-2-pyridinylbenzenesulfonamide
Biological Activity
Potent and selective BRD4 bromodomain inhibitor (Ki = 30 - 50 nM for the first bromodomain (BRD4(1)). Exhibits 10-fold selectivity for BRD4(1) over BRD4(2). Blocks BRD4 transcriptional activity in lipopolysaccharide-induced production of both nitric oxide and IL-6 in mouse macrophages (IC50 values are 3.8 and 4.9 μM, respectively). Attenuates melanoma cell proliferation in vitro.
Technical Data
  • M.Wt:
    383.42
  • Formula:
    C18H17N5O3S
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at -20°C
  • CAS No:
    1395084-25-9
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:
Sold under license from Icahn School of Medicine at Mount Sinai.
Background References
  1. Structure-guided design of potent diazobenzene inhibitors for the BET bromodomains.
    Zhang et al.
    J.Med.Chem., 2013;56:9251
  2. BRD4 sustains melanoma proliferation and represents a new target for epigenetic therapy.
    Segura et al.
    Cancer Res., 2013;73:6264

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