GSK8814
Product Specifications
Product Name Alternative
RU-42932
UNSPSC 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].
Target Antigen
Epigenetic Reader Domain
Type
Reference compound
Related Pathways
Epigenetics
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/gsk8814.html
Purity
99.60
Solubility
DMSO : 100 mg/mL (ultrasonic)
Smiles
O=C1NC2=C(N[C@H]3[C@H](OCC4CCC(F)(F)CC4)CNC[C@@H]3OC)N=CC(C5=CC(C)=CN=C5)=C2C=C1C
Molecular Weight
527.61
References & Citations
[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.
Shipping Conditions
Blue Ice
Storage Conditions
-20°C, 3 years (Powder)
Product Datasheet
http://file.medchemexpress.com/batch_PDF/HY-114204/GSK8814-DataSheet-MedChemExpress.pdf
Product MSDS
http://file.medchemexpress.com/batch_PDF/HY-114204/GSK8814-SDS-MedChemExpress.pdf
Clinical Information
No Development Reported
CAS Number
1997369-78-4
Available Sizes
Curated Selection
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