GSK-6853( GSK6853 )

Catalog No. M12992 CAS No. 1910124-24-1

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

GSK-6853
Note

Research use only, not for human use.
Brief Description

A potent, highly selective and cell-active BRPF1 bromodomain inhibitor with TR-FRET pIC50 of 8.1.
Description

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

——
In Vivo

The ip route of administration would be suitable for dosing GSK6853 in potential PK/PD models.
Synonyms

GSK6853
Pathway

Chromatin/Epigenetic
Target

Bromodomain
Recptor

BRPF1|BRPF2|BRPF3
Research Area

Cancer
Indication

——

CAS Number

1910124-24-1
Formula Weight

409.4815
Molecular Formula

C22H27N5O3
Purity

>98% (HPLC)
Solubility

DMSO: ≥ 29 mg/mL
SMILES

O=C(NC1=C(N2[C@H](C)CNCC2)C=C(N3C)C(N(C)C3=O)=C1)C4=CC=CC=C4OC
Chemical Name

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

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

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