GSK8814
- Product Name
- GSK8814
- CAS No.
- 1997369-78-4
- Chemical Name
- GSK8814
- Synonyms
- GSK8814;GSK8814,GSK-8814;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)-
- CBNumber
- CB23339891
- Molecular Formula
- C28H35F2N5O3
- Formula Weight
- 527.61
- MOL File
- 1997369-78-4.mol
GSK8814 Property
- form
- Solid
- color
- Light yellow to yellow
N-Bromosuccinimide Price
- Product number
- SML2111
- Product name
- GSK8814
- Purity
- ≥98% (HPLC)
- Packaging
- 5 mg
- Price
- $183
- Updated
- 2025/07/31
- Product number
- SML2111
- Product name
- GSK8814
- Purity
- ≥98% (HPLC)
- Packaging
- 25 mg
- Price
- $735
- Updated
- 2025/07/31
- Product number
- CS-0079595
- Product name
- GSK8814
- Packaging
- 5mg
- Price
- $300
- Updated
- 2021/12/16
- Product number
- CS-0079595
- Product name
- GSK8814
- Packaging
- 10mg
- Price
- $510
- Updated
- 2021/12/16
GSK8814 Chemical Properties,Usage,Production
Uses
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].
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].
IC 50
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.
GSK8814 Preparation Products And Raw materials
Raw materials
Preparation Products
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