| Identification | Back Directory | [Name]
GSK8814 | [CAS]
1997369-78-4 | [Synonyms]
GSK8814
1,7-Naphthyridin-2(1H)-one, 8-[[(3R,4R,5S)-3-[(4,4-difluorocyclohexyl)methoxy]-5-methoxy-4-piperidinyl]amino]-3-methyl-5-(5-methyl-3-pyridinyl)- | [Molecular Formula]
C28H35F2N5O3 | [MDL Number]
MFCD32867296 | [MOL File]
1997369-78-4.mol | [Molecular Weight]
527.61 |
| Hazard Information | Back Directory | [Uses]
GSK8814 is a potent, selective, and ATAD2/2B bromodomain chemical probe and inhibitor, with a binding constant pKd=8.1 and a pKi=8.9 in BROMOscan. GSK8814 binds to ATAD2 and BRD4 BD1 with pIC50s of 7.3 and 4.6, respectively. GSK8814 shows 500-fold selectivity for ATAD2 over BRD4 BD1[1]. | [Biological Activity]
GSK8814 is a potent, selective, and ATAD2/2B bromodomain chemical probe and inhibitor, with a binding constant pKd=8.1 and a pKi=8.9 in BROMOscan. GSK8814 binds to ATAD2 and BRD4 BD1 with pIC50s of 7.3 and 4.6, respectively. GSK8814 shows 500-fold selectivity for ATAD2 over BRD4 BD1[1]. | [IC 50]
ATAD2: 8.9 (pKi); ATAD2: 8 nM (Ki); BRD4 BD1: 4.6 (pIC50) | [References]
[1]. Bamborough P, et al. A Chemical Probe for the ATAD2 Bromodomain. Angew Chem Int Ed Engl. 2016 Sep 12;55(38):11382-6.
[2]. Bamborough P, et al. Aiming to Miss a Moving Target: Bromo and Extra Terminal Domain (BET) Selectivity in Constrained ATAD2 Inhibitors. J Med Chem. 2018 Sep 27;61(18):8321-8336. |
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