GSK 5959

Catalog #: 5385 Datasheet / COA / SDS

Discontinued Product

5385 has been discontinued.
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GSK 5959 | CAS No. 901245-65-6 | Bromodomain Inhibitors
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Description: Potent and selective BRPF1 inhibitor

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

Purity: ≥99%

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Biological Activity

GSK 5959 is a 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

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Background References

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

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