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GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain

Paul Bamborough, Heather A Barnett, Isabelle Becher, Mark J Bird, Chun-Wa Chung, Peter D Craggs, Emmanuel H Demont, Hawa Diallo, David J Fallon, Laurie J Gordon, Paola Grandi, Clare I Hobbs, Edward Hooper-Greenhill, etc.

ACS Med Chem Lett. 2016 May 9;7(6):552-7.

PMID: 27326325

Abstract:

The BRPF (Bromodomain and PHD Finger-containing) protein family are important scaffolding proteins for assembly of MYST histone acetyltransferase complexes. A selective benzimidazolone BRPF1 inhibitor showing micromolar activity in a cellular target engagement assay was recently described. Herein, we report the optimization of this series leading to the identification of a superior BRPF1 inhibitor suitable for in vivo studies.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP1910124241 GSK6853 GSK6853 1910124-24-1 Price
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