Chemical Name: N-[2,3-dihydro-1,3-dimethyl-6-[(2R)-2-methyl-1-piperazinyl]-2-oxo-1H-benzimidazol-5-yl]-2-methoxybenzamide
Biological ActivityPotent and selective BRPF1 inhibitor. Exhibits >1600-fold selectivity for BRPF1 over other bromodomains (pIC50 values by TR-FRET are 8.1, 5.1/4.8 and 4.7/<4.3 for BRPF1, BRPF2/3 and BRD4 BD1/2, respectively).
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.
GSK6853, a chemical probe for inhibition of the BRPF1 bromodomain.
Bamborough et al.
ACS Med.Chem.Lett., 2016;7:552
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