For research use only. Not for therapeutic Use.
GSK9311, a less active analogue of GSK6853, can be used as a negative control. GSK9311 inhibits BRPF bromodomain with pIC50 values of 6.0 and 4.3 for BRPF1 and BRPF2, respectively[1].
GSK6853 is a potent (300 pM), soluble, cell active (20 nM), and highly selective inhibitor of the BRPF1 bromodomain, and demonstrates properties suitable for cellular and in vivo studies. GSK6853 is a less active analogue of GSK6853 in which the 5-amide is alkylated[1].
| Catalog Number | I007127 |
| CAS Number | 1923851-49-3 |
| Synonyms | N-[1,3-dimethyl-6-[(2R)-2-methylpiperazin-1-yl]-2-oxobenzimidazol-5-yl]-N-ethyl-2-methoxybenzamide |
| Molecular Formula | C24H31N5O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C24H31N5O3/c1-6-28(23(30)17-9-7-8-10-22(17)32-5)20-13-18-19(27(4)24(31)26(18)3)14-21(20)29-12-11-25-15-16(29)2/h7-10,13-14,16,25H,6,11-12,15H2,1-5H3/t16-/m1/s1 |
| InChIKey | WFXIHQFRQPGCCR-MRXNPFEDSA-N |
| SMILES | CCN(C1=C(C=C2C(=C1)N(C(=O)N2C)C)N3CCNCC3C)C(=O)C4=CC=CC=C4OC |
| Reference | [1]. Bamborough P, et al. GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain. ACS Med Chem Lett. 2016 May 9;7(6):552-7. |
