| Identification | Back Directory | [Name]
GSK6853 | [CAS]
1910124-24-1 | [Synonyms]
GSK6853
CS-2243
GSK-6853;GSK 6853
GSK6853 >=98% (HPLC)
FQWDVNSBYDXPIO-CQSZACIVSA-N
BRPF1 bromodomain inhibitor GS6853
N-[2,3-dihydro-1,3-dimethyl-6-[(2R)-2-methyl-1-piperazinyl]-2-oxo-1H-benzimidazol-5-yl]-2-methoxybenzamide
Benzamide, N-[2,3-dihydro-1,3-dimethyl-6-[(2R)-2-methyl-1-piperazinyl]-2-oxo-1H-benzimidazol-5-yl]-2-methoxy- | [Molecular Formula]
C22H27N5O3 | [MDL Number]
MFCD30489734 | [MOL File]
1910124-24-1.mol | [Molecular Weight]
409.48 |
| Questions And Answer | Back Directory | [Uses]
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. |
| Chemical Properties | Back Directory | [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. |
| Hazard Information | Back Directory | [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. | [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 |
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