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GSK-J4

Chemical Structure : GSK-J4

CAS No.: 1373423-53-0

GSK-J4 (GSK-J4 hydrochloride)

Catalog No.: PC-21211Not For Human Use, Lab Use Only.

GSK-J4 is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively, GSK-J4 s a cell permeable prodrug of GSK-J1.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

GSK-J4 is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively, GSK-J4 s a cell permeable prodrug of GSK-J1.
GSK-J4 inhibits LPS-induced TNF-α production in human primary macrophages with IC50 of 9 uM.
GSK-J4 prevents the JMJD3-induced loss of nuclear H3K27me3 immunostaining in Flag-JMJD3-transfected HeLa cells.
GSK-J4 inhibits JMJD3 expression that is induced by TGF-β1, inhibits H3K4 demethylation at Xist, Nodal, and HoxC13 in female embryonic stem cells.
GSK-J4 attenuates the development of kidney disease in diabetic mice.

Physicochemical Properties

M.Wt 453.97
Formula C24H28ClN5O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate hydrochloride

References

1. Kruidenier L, et al. Nature. 2012 Aug 16;488(7411):404-8.

2. Majumder S, et al. J Clin Invest. 2018 Jan 2;128(1):483-499.

3. Donas C, et al. J Autoimmun. 2016 Dec;75:105-117.

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