GSK J4 is an ethyl ester derivative of GSK J1, which is a potent 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 is a potent cell-permeable inhibitor of the histone H3 lysine 27 (H3K27) demethylase JMJD3, an essential component of regulatory transcriptional chromatin complexes, with the half-maximal inhibition concentration IC50 value >50 μM in vitro. GSK J4 has also been found to dose-dependently inhibit the production of tumor-necrosis factor-α (TNF-α), and LPS-driven cytokine involved in various inflammatory disorders (IC50: 9μM) [1].

T22819

C24H27N5O2·HCl

453.96

GSK J4 HCl;GSK J4 HCl (1373423-53-0 free base)

Ethanol:<1 mgml
DMSO:≥13.9 mg/mL
H2O:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years