WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406745
Description: GSK6853 is a potent (300 pM), soluble, cell active (20 nM), and highly selective inhibitor of the BRPF1 bromodomain, and demonstrated properties suitable for cellular and in vivo studies. The BRPF (Bromodomain and PHD Fingercontaining) protein family are important scaffolding proteins for assembly of MYST histone acetyltransferase complexes. BRPF1 (bromodomain and PHD finger containing protein 1) is involved in the epigenetic regulation of gene expression and have been implicated in human cancer.
MedKoo Cat#: 406745
Chemical Formula: C22H27N5O3
Exact Mass: 409.2114
Molecular Weight: 409.49
Elemental Analysis: C, 64.53; H, 6.65; N, 17.10; O, 11.72
Synonym: GSK6853; GSK 6853; GSK-6853.
IUPAC/Chemical Name: (R)-N-(1,3-dimethyl-6-(2-methylpiperazin-1-yl)-2-oxo-2,3-dihydro-1H-benzo[d]imidazol-5-yl)-2-methoxybenzamide
InChi Key: FQWDVNSBYDXPIO-CQSZACIVSA-N
InChi Code: InChI=1S/C22H27N5O3/c1-14-13-23-9-10-27(14)17-12-19-18(25(2)22(29)26(19)3)11-16(17)24-21(28)15-7-5-6-8-20(15)30-4/h5-8,11-12,14,23H,9-10,13H2,1-4H3,(H,24,28)/t14-/m1/s1
SMILES Code: O=C(NC1=C(N2[C@H](C)CNCC2)C=C(N3C)C(N(C)C3=O)=C1)C4=CC=CC=C4OC
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, Emma J. Jones, Robert P. Law, Armelle Le Gall, David Lugo, Anne-Marie Michon, Darren J. Mitchell, Rab K. Prinjha, Robert J. Sheppard, Allan J. B. Watson, and Robert J. Watson
Publication Date (Web): May 9, 2016 (Featured Letter)