1997369-78-4

1997369-78-4 structure

Name: GSK8814
Chemical Name: GSK8814
CAS Number: 1997369-78-4
Molecular Formula: C₂₈H₃₅F₂N₅O₃
Molecular Weight: 527.61
Catalog: Signaling Pathways Epigenetics Epigenetic Reader Domain
Create Date: 2018-06-21 08:29:19
Modify Date: 2024-01-12 19:09:41
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].

Name	GSK8814

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.

Molecular Formula	C₂₈H₃₅F₂N₅O₃
Molecular Weight	527.61