GSK J4 HCl

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.
Synonym(s): ethyl 3-[[2-pyridin-2-yl-6-(1,2,4,5-tetrahydro-3-benzazepin-3-yl)pyrimidin-4-yl]amino]propanoate
Purity: ≥98% by HPLC
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).
Solubility: Soluble in DMSO 84 mg/ml, water 84 mg/ml, ethanol 84 mg/ml
Storage / Stability: Store at or below –20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.
Reference(s): Kruidenier L, et al. Nature. 2012 Aug 16;488(7411):404-8.
Scientific Category: Demethylase(s)
Product Type: Inhibitors / Activators