GSK8814( GSK 8814 | GSK-8814 )

Catalog No. M13118 CAS No. 1997369-78-4

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

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Product Name

GSK8814
Note

Research use only, not for human use.
Brief Description

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

GSK8814 is a potent, selective inhibitor of ATAD2/2B bromodomain binding constant pKd of 8.1 in ITC assays; displaces acetylated H4 peptide from the ATAD2 bromodomain with pIC50 of 7.3 and is also active in BROMOscan with pKi of 8.9, displays >100 fold selective over all other bromodomains and >1,000 fold selective over BRD4; 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.
In Vitro

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In Vivo

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Synonyms

GSK 8814 | GSK-8814
Pathway

Chromatin/Epigenetic
Target

Bromodomain
Recptor

Bromodomain
Research Area

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Indication

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CAS Number

1997369-78-4
Formula Weight

527.617
Molecular Formula

C28H35F2N5O3
Purity

>98% (HPLC)
Solubility

In Vitro:?DMSO : 100 mg/mL (189.53 mM)
SMILES

CC(C(N1)=O)=CC2=C1C(N[C@H]3[C@H](OCC4CCC(F)(F)CC4)CNC[C@@H]3OC)=NC=C2C5=CN=CC(C)=C5
Chemical Name

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