Name: GSK6853
Price: 294.00 USD

- Overview
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    Background
    
    pIC50: 8.1GSK6853 is a BRPF1 inhibitor.The BRPF (Bromodomain and PHD Fingercontaining) protein family are key scaffolding proteins for assembly of MYST histone acetyltransferase complexes.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].Clinical trial: So far, no clinical study has been conducted.
- Properties
  - Alternative Name
    
    N-[2,3-dihydro-1,3-dimethyl-6-[(2R)-2-methyl-1-piperazinyl]-2-oxo-1H-benzimidazol-5-yl]-2-methoxy-benzamide
    
    CAS Number
    
    1910124-24-1
    
    Molecular Formula
    
    C22H27N5O3
    
    Molecular Weight
    
    409.5
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≤30mg/ml in ethanol;25mg/ml in DMSO;30mg/ml in dimethyl formamide
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only