Catalog Number: 6181
Chemical Name: (6S)-4-(4-Chlorophenyl)-N-(4-hydroxyphenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide
Biological Activity
BET bromodomain inhibitor (IC50 values are in the range 92 - 112 nM). Inhibits proliferation and induces apoptosis of leukemia cell lines in vitro. Decreases BRD2, BRD4 and c-MYC protein expression. Orally bioavailable.
Technical Data
  • M.Wt:
    491.99
  • Formula:
    C25H22ClN5O2S
  • Solubility:
    Soluble to 100 mM in DMSO and to 20 mM in ethanol
  • Purity:
    >98%
  • Storage:
    Store at -20°C
  • CAS No:
    202590-98-5
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. OTX015 (MK-8628), a novel BET inhibitor, displays in vitro and in vivo antitumor effects alone and in combination with conventional therapies in glioblastoma models.
    Berenguer-Daizé et al.
    Int.J.Cancer, 2016;139:2047
  2. BET inhibitor OTX015 targets BRD2 and BRD4 and decreases c-MYC in acute leukemia cells.
    Coudé et al.
    Oncotarget, 2015;6:17698
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