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GSK-6853

Chemical Structure : GSK-6853

CAS No.: 1910124-24-1

GSK-6853 (GSK6853)

Catalog No.: PC-42090Not For Human Use, Lab Use Only.

GSK-6853 (GSK6853) is a potent, highly selective and cell-active BRPF1 bromodomain inhibitor with TR-FRET pIC50 of 8.1.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

GSK-6853 (GSK6853) is a potent, highly selective and cell-active BRPF1 bromodomain inhibitor with TR-FRET pIC50 of 8.1.
GSK-6853 displays>1600-fold selectivity over others bromodomains (BRPF2/3, BRD4 BD1/BD2).
GSK-6853 displaces NanoLuc-tagged BRPF1 bromodomain from Halo-tagged histone H3.3 (IC50=20 nM) and disrupts chromatin binding in cell assays.
GSK-6853 demonstrates properties suitable for cellular and in vivo studies.

Physicochemical Properties

M.Wt 409.4815
Formula C22H27N5O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 29 mg/mL

Chemical Name/SMILES

Benzamide, N-[2,3-dihydro-1,3-dimethyl-6-[(2R)-2-methyl-1-piperazinyl]-2-oxo-1H-benzimidazol-5-yl]-2-methoxy-

References

1. Bamborough P, et al. ACS Med Chem Lett. 2016 May 9;7(6):552-7.

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