Synonyms: 8-((3R,4R,5S)-3-((4,4-Difluorocyclohexyl)methoxy)-5-methoxypiperidin-4-ylamino)-3-methyl-5-(5-methylpyridin-3-yl)-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)-1,7-naphthyridin-2(1H)-one
Molecular Formula: C28H35F2N5O3
Molecular Weight: 527.61
Linear Structural Formula: C28H35F2N5O3
Purity: >=98% (HPLC)
Storage: -20C
Biochem Physiol Actions: GSK8814 is an aqueous soluble (>439 muM) inhibitor that targets ATAD2 & ATAD2B bromodomain (BD) with submicromolar affinity (pKd = 8.1 for ATAD2 by ITC) and high selectivity (pIC50 = 7.3/ATAD2 BD & 7.7/ATAD2B BD in competitive ligand binding assays by TR-FRET; pIC50 <=4.5 when using BD1/BD2 of BRD2-4 or BRDT). When tested using intact cells, GSK8814 effectively disrupts histone H3.3 interaction with ATAD2 BD construct (IC50 = 2.7 muM), but not full-length ATAD2. GSK8814, but not its less active diastereomer GSK8815, is shown to suppress LNCaP colony formation in a soft agar assay, albeit with a high effective concentration (by 56% at 20 muM).