GSK-J4,H3K27HistoneDemethylasesUTXandJMJD3Inhibitor

GSK-J4 is an ethyl ester derivative of GSK-J1, which is the first selective and potent inhibitor of the H3K27 histone demethylases UTX and JMJD3. The highly polar carboxylate group of GSK-J1 restricts its cellular permeability, therefore GSK-J4 was developed as a pro-drug, masking the polarity of the acid group of the GSK-J1, for cellular assays. GSK-J4 could significant reduce LPS-induced pro-inflammatory cytokine production in primary human macrophages (IC₅₀ ~9 μM for the inhibition of TNFα release). Together with GSK-J1, GSK-J4 could be a unique small molecule to allow selective pharmacological intervention across the JMJ family.

How to Use:

• In vitro:  GSK-J4 was used at 30 µM final concentration in cellular assays.
• In vivo: n/a

Reference:

• 1. Kruidenier L, et al. A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response (2012) Nature. 488(7411):404-8.
• 2. SGC website: http://www.thesgc.org/scientists/chemical_probes/GSKJ1 

Products are for research use only. Not for human use.