GSK6853

• CAT Number: I002449
• CAS Number: 1910124-24-1
• Molecular Formula: C22H27N5O3
• Molecular Weight: 409.5
• Purity: ≥95%
• Target: Bromodomain
• Solubility: DMSO ≥ 31 mg/mL
• Storage: Store at -20°C
• IUPAC Name: N-[1,3-dimethyl-6-[(2R)-2-methylpiperazin-1-yl]-2-oxobenzimidazol-5-yl]-2-methoxybenzamide
• InChI: 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
• InChIKey: FQWDVNSBYDXPIO-CQSZACIVSA-N
• SMILES: CC1CNCCN1C2=CC3=C(C=C2NC(=O)C4=CC=CC=C4OC)N(C(=O)N3C)C

GSK6853（Cat No.:I002449） is a potent and selective RPF1 acetyllysine inhibitor (pKd=9.5), with 1600-fold selectivity over other acetyllysines. GSK6853 can be used to prepare bromodomain and PHD finger-containing protein inhibitors for biological research.

Reference

1:ACS Med Chem Lett. 2016 May 9;7(6):552-7. doi: 10.1021/acsmedchemlett.6b00092. eCollection 2016 Jun 9. GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain.Bamborough P,Barnett HA,Becher I,Bird MJ,Chung CW,Craggs PD,Demont EH,Diallo H,Fallon DJ,Gordon LJ,Grandi P,Hobbs CI,Hooper-Greenhill E,Jones EJ,Law RP,Le Gall A,Lugo D,Michon AM,Mitchell DJ,Prinjha RK,Sheppard RJ,Watson AJ,Watson RJ, PMID: 27326325 PMCID: PMC4904261 [Available on 2017-06-09] DOI: 10.1021/acsmedchemlett.6b00092 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.