GSK8814

Names

[ CAS No. ]:
1997369-78-4

[ Name ]:
GSK8814

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain

[Target]

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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₈H₃₅F₂N₅O₃

[ Molecular Weight ]:
527.61

Related Compounds

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