GSK-J4 hydrochloride 是H3K27me3/me2 去甲基化酶JMJD3/KDM6B和UTX/KDM6A双抑制剂，IC50分别为 8.6 和 6.6 μM。它是 GSK-J1 的乙酯衍生物，体外 IC50 值大于 50 μM。它抑制 LPS 诱导的人原代巨噬细胞产生 TNF-α，IC50值为 9 μM。

GSK-J4 is a cell permeable, potent and selective histone demethylase(JMJD3 )inhibitor. is an ethyl ester derivative of the GSK-J1 with an IC50 value greater than 50 μM in vitro.

When administered to human primary macrophages, GSK-J4 can reduce LPS-induced proinflammatory cytokine production, most notably including that of TNFα (IC50 = 9 μM).

Acting as a prodrug, GSK-J4 is rapidly hydrolyzed in cells to the otherwise cell impermeable GSK-J1, which exhibits an IC50 value of 60 nM for the purified enzyme. The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.

1797983-09-5

C24H28ClN5O2

453.97

GSK J4 HCl

DMSO:30 mg/mL
Ethanol:20 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years