GSK5959, BRPF1 Bromodomain Inhibitor


Catalog No. size PriceQuantity
M60239-2S 2 mg solid $129
M60239-10S 10mg solid $536

Description

Product Information
Molecular Weight: 394.47
Formula: C22H26N4O3
Purity: ≥98%
CAS#: 901245-65-6
Solubility: DMSO up to 10 mM
Chemical Name: N-(1,3-dimethyl-2-oxo-6-(piperidin-1-yl)-2,3-dihydro-1H-benzo[d]imidazol-5-yl)-2-methoxybenzamide
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

 

Biological Activity:

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

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):1190-5.

Products are for research use only. Not for human use. 

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