GSK8814 |
| Catalog No.GC60184 |
GSK8814는 BROMOscan에서 결합 상수 pKd=8.1 및 pKi=8.9를 갖는 강력하고 선택적인 ATAD2/2B 브로모도메인 화학 프로브 및 억제제입니다. GSK8814는 각각 7.3 및 4.6의 pIC50으로 ATAD2 및 BRD4 BD1에 결합합니다. GSK8814는 BRD4 BD1에 비해 ATAD2에 대해 500배 선택성을 보여줍니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1997369-78-4
Sample solution is provided at 25 µL, 10mM.
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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.
Average Rating: 5 (Based on Reviews and 38 reference(s) in Google Scholar.)
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