The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer. GSK-J4 is a cell-permeable prodrug which is modified by intracellular esterases to give GSK-J1 , an inhibitor of JMJD3. GSK-J5 is a pyridine regio-isomer of GSK-J4. Like GSK-J4, this isomer is cell-permeable and hydrolyzed to a free base. However, the free base is a weak inhibitor of JMJD3 (IC50 >100 μM), making it an ideal inactive control molecule for elucidating the functional role of JMJD3 inhibition.

1797983-32-4

C24H28ClN5O2

453.96

GSK-J5 (hydrochloride);GSK-J5 hydrochloride

DMSO:30 mg/mL
DMF:30 mg/mL
DMF:PBS (pH 7.2)(1:7):0.1 mg/mL
Ethanol:20 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years