GSK-J5 (hydrochloride)

The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.{19496,19494} GSK-J4 (Item No. 12073) is a cell-permeable prodrug which is modified by intracellular esterases to give GSK-J1 (Item No. 12054), 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.{21388} However, the free base is a weak inhibitor of JMJD3 (IC50 > 100 ?M), making it an ideal inactive control molecule for elucidating the functional role of JMJD3 inhibition.{21388}