GSK8814

GSK8814 is a potent and selective ATAD2 bromodomain chemical probe and inhibitor (IC50 = 0.059 μM), 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. GSK8814 can be researched for cancer associated with ATAD2 bromodomain[1][2][3].

Product Specifications

CAS Number

[1997369-78-4]

Product Name Alternative

RU-42932

UNSPSC

12352005

Target

Epigenetic Reader Domain

Type

Reference compound

Related Pathways

Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/gsk8814.html

Purity

99.80

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 Formula

C28H35F2N5O3

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.|[3]Yao, D., et al., (2023) . Fragment-based design, synthesis and biological evaluation of theophylline derivatives as ATAD2 inhibitors in BT-549 cells. Journal of enzyme inhibition and medicinal chemistry, 38 (1), 2242601.