GSK8814

Modify Date: 2024-01-12 19:09:41

GSK8814 Structure
GSK8814 structure
Common Name GSK8814
CAS Number 1997369-78-4 Molecular Weight 527.61
Density N/A Boiling Point N/A
Molecular Formula C28H35F2N5O3 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of GSK8814


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].

 Names

Name GSK8814

 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
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
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