Chemical Name: (4S)-6-(4-Chlorophenyl)-N-ethyl-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine-4-acetamide
Biological ActivityPotent and high affinity BET bromodomain inhibitor (IC50 = 32.5 - 42.5 nM; Kd = 50.5 - 61.3 nM). Inhibits myeloma cell proliferation. Attenuates transcription of oncogenic MYC and suppresses key inflammatory genes. Exhibits efficacy in a range of oncology and immunoinflammatory models. Displays antiproliferative effect in vitro and in vivo. Orally bioavailable.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762.
Chaidos et al.
Discovery of epigenetic regulator I-BET762: lead optimization to afford a clinical candidate inhibitor of the BET bromodomains.
Mirguet et al.
Suppression of inflammation by a synthetic histone mimic.
Nicodeme et al.
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