GSK8814 | ATAD2/2B inhibitor | Probechem Biochemicals

Chemical Structure : GSK8814

CAS No.: 1997369-78-4

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GSK8814 (GSK 8814, GSK-8814)

货号: PC-63576Not For Human Use, Lab Use Only.

GSK8814 is a potent, selective inhibitor of ATAD2/2B bromodomain binding constant pKd of 8.1 in ITC assays.

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5 mg	￥3580	In stock
10 mg	￥5580	In stock
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生物&药学活性

GSK8814 is a potent, selective inhibitor of ATAD2/2B bromodomain binding constant pKd of 8.1 in ITC assays.
GSK8814 displaces acetylated H4 peptide from the ATAD2 bromodomain with pIC50 of 7.3 and is also active in BROMOscan with pKi of 8.9.
GSK8814 displays >100 fold selective over all other bromodomains and >1,000 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.

物理化学性质&存储条件

分子量	527.617
分子式	C28H35F2N5O3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	8-(((3R,4R,5S)-3-((4,4-difluorocyclohexyl)methoxy)-5-methoxypiperidin-4-yl)amino)-3-methyl-5-(5-methylpyridin-3-yl)-1,7-naphthyridin-2(1H)-one

参考文献

1. Bamborough P, et al. Angew Chem Int Ed Engl. 2016 Sep 12;55(38):11382-6.

GSK8814 (GSK 8814, GSK-8814)

生物&药学活性

物理化学性质&存储条件

参考文献

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GSK8814 (GSK 8814, GSK-8814)

生物&药学活性

物理化学性质&存储条件

参考文献

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