GSK6853

Synonym(s):(R)-N-(1,3-Dimethyl-6-(2-methylpiperazin-1-yl)-2-oxo-2,3-dihydro-1H-benzo[d]imidazol-5-yl)-2-methoxybenzamide;N-[2,3-Dihydro-1,3-dimethyl-6-[(2R)-2-methyl-1-piperazinyl]-2-oxo-1H-benzimidazol-5-yl]-2-methoxybenzamide

CAS NO.：1910124-24-1
Empirical Formula: C22H27N5O3
Molecular Weight: 409.48
MDL number: MFCD30489734
Update Date: 2024-11-15 21:27:52

What is GSK6853?

Description

GSK6853 (1910124-24-1) is a very potent (pIC50 = 8.6 vs full length protein, 7.7 in cellular assays) inhibitor of Bromodomain and PHD Finger-containing 1 (BRPF1). It displayed >1600-fold selectivity over other bromodomains.

The Uses of GSK6853

N-[2,3-Dihydro-1,3-dimethyl-6-[(2R)-2-methyl-1-piperazinyl]-2-oxo-1H-benzimidazol-5-yl]-2-methoxybenzamide can be used in biological study of preparation of bromodomain and PHD finger-containing protein inhibitors.

in vitro

in previous study, gsk6853 was tested in the bromoscan panel of bromodomain binding assays and the results showed that consistent with the previous findings, it showed excellent brpf1 potency (pkd 9.5) and greater than 1600-fold selectivity over all other bromodomains tested. in addition, screening gsk6853 against a panel of 48 unrelated assays revealed only off-target activities that were relatively weak compared to its high brpf1 potency [1].

in vivo

to assess the suitability of gsk6853 for in vivo studies, its dmpk characteristics were studied in male cd1 mice by i.v., po, and i.p. administration. the results indicated that the i.p. route of administration would be suitable for dosing this molecule in further pk/pd models. moreover, in order to be able to compare biochemical potency measurements to free blood concentrations, the fraction unbound in the cd1 mouse was also tested with a resulting value of 7.9% [1].

storage

Store at -20°C

References

Bamborough et al. (2016), GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain; ACS Med.Chem. Lett. 7 552

Properties of GSK6853

Boiling point:	545.9±50.0 °C(Predicted)
Density	1.247±0.06 g/cm3(Predicted)
storage temp.	Sealed in dry,Store in freezer, under -20°C
solubility	Soluble in DMSO (25 mg/ml); ethanol (25 mg/ml)
form	solid
pka	13.03±0.20(Predicted)
color	White
Stability:	Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.