|Solubility:||DMSO up to 10 mM|
|Storage:||Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.|
GSK5959 is a potent, selective and cell permeable BRPF1 bromodomain inhibitor with IC50 ~ 80 nM. It has >100-fold selectivity for BRPF1 over a panel of 35 other bromodomains, including BRPF2/3 and BET family bromodomains. A cellular protein interaction assay measuring the displacement of NanoLuc-tagged BRPF1 bromodomain from Halotagged histone H3.3 was employed to demonstrate GSK5959’s cell permeability and disruption of chromatin binding with IC50 ~0.98 µM.
How to Use:
In vitro: GSK5959 was used at 10 µM final concentration in various in vitro assays.
In vivo: n/a
- 1. Demont EH, et al. 1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain. (2014) ACS Med Chem Lett. 5(11):1190-5.
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