GSK8814 is a chemical probe for the ATAD2/2B bromodomain, with a binding constant pKd=8.1 as measured by ITC (Bamborough et al, 2016). GSK8814 displaces acetylated H4 peptide from the ATAD2 bromodomain with pIC50 =7.3 and is also active in BROMOscan with pKi=8.9. It is more than 100 fold selective over all other bromodomains in the BROMOscan. Importantly, it is more than 1000 fold selective over BRD4. GSK8814 shows cellular target engagement with an EC50 of 2 µM in a NanoBRET assay evaluating the interaction of the NanoLuc-ATAD2 bromodomain with histone H3.3-HaloTag. GSK8815 is a companion control compound with strongly reduced potency against ATAD2 (pKd=5.5). (http://www.thesgc.org/chemical-probes/GSK8814)
MedKoo Cat#: 407419
Name: GSK8814
CAS#: 1997369-78-4
Chemical Formula: C28H35F2N5O3
Exact Mass: 527.2708
Molecular Weight: 527.62
Elemental Analysis: C, 63.74; H, 6.69; F, 7.20; N, 13.27; O, 9.10
The following data is based on the product molecular weight 527.62 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
