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GSK-J1 lithium salt

Catalog No. T11475   CAS 2309668-29-7

GSK-J1 lithium salt is an effective inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with an IC 50 of 60 nM for KDM6B.

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GSK-J1 lithium salt Chemical Structure
GSK-J1 lithium salt, CAS 2309668-29-7
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Biological Description
Chemical Properties
Storage & Solubility Information
Description GSK-J1 lithium salt is an effective inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with an IC 50 of 60 nM for KDM6B.
Targets&IC50 KDM6B:60 nM
In vitro GSK-J1 is selective for H3K27 demethylases of the KDM6 subfamily and specifically binds to endogenous JMJD3. GSK-J1 inhibits TNF-α production by human primary macrophages in an H3K27-dependent manner [1]. GSK-J1 inhibits the demethylase activity of KDM5C with 8.5-fold increased potency than that of KDM5B at 1 mM α-ketoglutarate, with IC 50 of 11 μM and 94 μM, respectively [3].
Molecular Weight 395.38
Formula C22H22LiN5O2
CAS No. 2309668-29-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. Kruidenier L, et al. A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response. Nature. 2012 Aug 16;488(7411):404-8. 2. Heinemann B, et al. Inhibition of demethylases by GSK-J1/J4. Nature. 2014 Oct 2;514(7520):E1-2. 3. Horton JR, et al. Characterization of a Linked Jumonji Domain of the KDM5/JARID1 Family of Histone H3 Lysine 4 Demethylases. J Biol Chem. 2016 Feb 5;291(6):2631-46.

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Keywords

GSK-J1 lithium salt 2309668-29-7 Chromatin/Epigenetic Histone Demethylase GSKJ1 lithium salt GSK-J1 lithium GSK-J-1 lithium salt GSK J1 lithium salt inhibitor inhibit

 

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