GSK8814 |
カタログ番号GC60184 |
GSK8814 は、強力で選択的な ATAD2/2B ブロモドメイン化学プローブおよび阻害剤であり、BROMOscan で結合定数 pKd=8.1 および pKi=8.9 を持っています。 GSK8814 は、ATAD2 および BRD4 BD1 にそれぞれ pIC50 7.3 および 4.6 で結合します。 GSK8814 は、BRD4 BD1 よりも ATAD2 に対して 500 倍の選択性を示します。
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Cas No.: 1997369-78-4
Sample solution is provided at 25 µL, 10mM.
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].
[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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