For research use only. Not for therapeutic Use.
GSK8814(CAT: I006837) is a potent, selective chemical probe and inhibitor of the ATAD2/ATAD2B bromodomains, with strong binding affinity (pKᵈ = 8.1; pKᵢ = 8.9, BROMOscan). It exhibits high selectivity, binding ATAD2 with a pIC₅₀ of 7.3 while showing significantly weaker activity against BRD4 BD1 (pIC₅₀ = 4.6), achieving over 500-fold selectivity for ATAD2 versus BRD4. As a first-in-class probe, GSK8814 provides a powerful tool for investigating the role of ATAD2 in chromatin biology, gene regulation, and cancer progression. Its high potency and selectivity make it valuable for validating ATAD2 as a therapeutic target in oncology and epigenetic research.
| CAS Number | 1997369-78-4 |
| Synonyms | 8-[[(3R,4R,5S)-3-[(4,4-difluorocyclohexyl)methoxy]-5-methoxypiperidin-4-yl]amino]-3-methyl-5-(5-methylpyridin-3-yl)-1H-1,7-naphthyridin-2-one |
| Molecular Formula | C28H35F2N5O3 |
| Purity | ≥95% |
| IUPAC Name | 8-[[(3R,4R,5S)-3-[(4,4-difluorocyclohexyl)methoxy]-5-methoxypiperidin-4-yl]amino]-3-methyl-5-(5-methylpyridin-3-yl)-1H-1,7-naphthyridin-2-one |
| InChI | InChI=1S/C28H35F2N5O3/c1-16-8-19(11-31-10-16)21-12-33-26(24-20(21)9-17(2)27(36)35-24)34-25-22(37-3)13-32-14-23(25)38-15-18-4-6-28(29,30)7-5-18/h8-12,18,22-23,25,32H,4-7,13-15H2,1-3H3,(H,33,34)(H,35,36)/t22-,23+,25+/m0/s1 |
| InChIKey | YDPMMWAOCCOULO-JBRSBNLGSA-N |
| SMILES | CC1=CC(=CN=C1)C2=CN=C(C3=C2C=C(C(=O)N3)C)NC4C(CNCC4OCC5CCC(CC5)(F)F)OC |
| Chemistry Calculators | Dilution Calculator In vivo Formulation Calculator Molarity Calculator Molecular Weight Calculator Reconstitution Calculator |
