1910124-24-1 Usage
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.
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].
References
Bamborough et al. (2016), GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain; ACS Med.Chem. Lett. 7 552
Check Digit Verification of cas no
The CAS Registry Mumber 1910124-24-1 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,9,1,0,1,2 and 4 respectively; the second part has 2 digits, 2 and 4 respectively.
Calculate Digit Verification of CAS Registry Number 1910124-24:
(9*1)+(8*9)+(7*1)+(6*0)+(5*1)+(4*2)+(3*4)+(2*2)+(1*4)=121
121 % 10 = 1
So 1910124-24-1 is a valid CAS Registry Number.
1910124-24-1Relevant articles and documents
GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain
Bamborough, Paul,Barnett, Heather A.,Becher, Isabelle,Bird, Mark J.,Chung, Chun-Wa,Craggs, Peter D.,Demont, Emmanuel H.,Diallo, Hawa,Fallon, David J.,Gordon, Laurie J.,Grandi, Paola,Hobbs, Clare I.,Hooper-Greenhill, Edward,Jones, Emma J.,Law, Robert P.,Le Gall, Armelle,Lugo, David,Michon, Anne-Marie,Mitchell, Darren J.,Prinjha, Rab K.,Sheppard, Robert J.,Watson, Allan J. B.,Watson, Robert J.
, p. 552 - 557 (2016/07/06)
The BRPF (Bromodomain and PHD Finger-containing) protein family are important scaffolding proteins for assembly of MYST histone acetyltransferase complexes. A selective benzimidazolone BRPF1 inhibitor showing micromolar activity in a cellular target engag
