GSK-J4 --- H3K27 Histone Demethylases UTX and JMJD3 Inhibitor

Bioss

GSK-J4 --- H3K27 Histone Demethylases UTX and JMJD3 Inhibitor [1373423-53-0]

16

Research Use Only

98.0

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 microM for the inhibition of TNFalpha release). Together with GSK-J1, GSK-J4 could be a unique small molecule to allow selective pharmacological intervention across the JMJ family.

-20°C

51202000