GSK J4 HCl
Catalog #
27627-2
$445
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Description
GSK J4 HCl is a cell permeable prodrug of GSK J1, which is the first selective inhibitor of the H3K27 histone demethylase JMJD3 and UTX with IC50 of 60 nM and inactive against a panel of demethylases of the JMJ family.
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Synonyms
ethyl 3-[[2-pyridin-2-yl-6-(1,2,4,5-tetrahydro-3-benzazepin-3-yl)pyrimidin-4-yl]amino]propanoate
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Product Data Gallery
Product Info
Storage and Usage
Citations
Purity
≥98% by HPLC
Target(s)
JMJD3, UTX
Formula
C24H27N5O2 • HCl
MW
454 Da
Solubility
Soluble in DMSO 84 mg/ml, water 84 mg/ml, ethanol 84 mg/ml
Biological Activity
Inhibits JMJD3 and UTX with IC50 of 60 nM and inactive against a panel of demethylases of the JMJ family (IC50 value > 50 µM).
CAS Registry #
1373423-53-0
Background
GSK J4 is a potent cell-permeable inhibitor of the histone H3 lysine 27 (H3K27) demethylase JMJD3. GSK J4 is an ethyl ester derivative of GSK J1, a JMJD3 inhibitor (IC50= 60 nM) with restricted cellular permeability due to the highly polar carboxylate group, and rapidly hydrolyzed by macrophage esterase upon administration leading to the generation of pharmacologically relevant intracellular concentration of GSK-J1 . GSK J4 has been found to dose-dependently inhibit the production of tumor-necrosis factor-α (TNF-α), a LPS-driven cytokine involved in various fnflammatory disorders (IC50 = 9 µM).
References
Kruidenier L, et al. Nature. 2012 Aug 16;488(7411):404-8.
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