GSK 5959

Cat. No. 5385

GSK 5959 C22H26N4O3 [901245-65-6]

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Chemical Name: N-[2,3-Dihydro-1,3-dimethyl-2-oxo-6-(1-piperidinyl)-1H-benzimidazol-5-yl]-2-methoxybenzamide

Biological Activity

Potent and selective BRPF1 bromodomain inhibitor (IC50 = 80 nM). Exhibits >100-fold selectivity for BRPF1 over a panel of 35 other bromodomains, including BRPF2/3 and BET family bromodomains. Inhibits BRPF1 interaction with histone H3.3. Cell permeable.

External Portal Information

Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of GSK 5959 is reviewed on the chemical probes website.

Technical Data

M.Wt:
394.47
Formula:
C22H26N4O3
Solubility:
Soluble to 10 mM in DMSO with sonication
Purity:
>99 %
Storage:
Store at +4°C
CAS No:
901245-65-6

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

Demont et al (2014) 1,3-dimethyl benzimidazolones are potent, selective inhibitors of the BRPF1 bromodomain. ACS Med.Chem.Lett. 5 1190. PMID: 25408830.

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Keywords: GSK 5959, supplier, GSK5959, potent, selective, BRPF1, bromodomains, inhibitors, inhibits, cell, permeable, Tocris Bioscience, Bromodomain Inhibitor products

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