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| GSK8814 Basic information |
Product Name: | GSK8814 | Synonyms: | GSK8814;1,7-Naphthyridin-2(1H)-one, 8-[[(3R,4R,5S)-3-[(4,4-difluorocyclohexyl)methoxy]-5-methoxy-4-piperidinyl]amino]-3-methyl-5-(5-methyl-3-pyridinyl)-;GSK8814,GSK-8814 | CAS: | 1997369-78-4 | MF: | C28H35F2N5O3 | MW: | 527.61 | EINECS: | | Product Categories: | | Mol File: | 1997369-78-4.mol | ![GSK8814 Structure](CAS/20180906/GIF/1997369-78-4.gif) |
| GSK8814 Chemical Properties |
form | Solid | color | Light yellow to yellow |
| GSK8814 Usage And Synthesis |
Biological Activity | 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]. | 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. |
| GSK8814 Preparation Products And Raw materials |
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