For research use only. Not for therapeutic Use.
GSK-5959 is a potent, selective and cell permeable BRPF1 bromodomain inhibitor with an IC50 of ~ 80 nM[1].
GSK-5959 (3a) also displays selectivity over the closely related family members, BRPF2 (100-fold) and BRPF3 (>1000-fold)[2].
GSK-5959 (3a) exhibits an EC50 = 0.98 μM) in cellular NanoBRET assay[2].
GSK-5959 has no effect on TRIM24 SUMOylation[3].
| Catalog Number | I005397 |
| CAS Number | 901245-65-6 |
| Synonyms | N-(1,3-dimethyl-2-oxo-6-piperidin-1-ylbenzimidazol-5-yl)-2-methoxybenzamide |
| Molecular Formula | C22H26N4O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C22H26N4O3/c1-24-18-13-16(23-21(27)15-9-5-6-10-20(15)29-3)17(26-11-7-4-8-12-26)14-19(18)25(2)22(24)28/h5-6,9-10,13-14H,4,7-8,11-12H2,1-3H3,(H,23,27) |
| InChIKey | LTUGYAOMCKNTGG-UHFFFAOYSA-N |
| SMILES | CN1C2=C(C=C(C(=C2)NC(=O)C3=CC=CC=C3OC)N4CCCCC4)N(C1=O)C |
| Reference | [1]. Demont EH, et al. 1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain. (2014) ACS Med Chem Lett. 5(11):1190-1195. [2]. Wylie S.Palmer, et al. Development of small molecule inhibitors of BRPF1 and TRIM24 bromodomains Discovery Today: Technologies Volume 19, March 2016, Pages 65-71. [3]. Srikanth Appikonda, et al. Cross-talk between chromatin acetylation and SUMOylation of tripartite motif-containing protein 24 (TRIM24) impacts cell adhesionJ Biol Chem. 2018 May 11;293(19):7476-7485. |
