4-Pyridinecarboxylic acid, 2-[[[2-[[2-(dimethylamino)ethyl]ethylamino]-2-oxoethyl]amino]methyl]-, 2,4-bis(1-methylethoxy)phenyl ester, hydrochloride (1:2)

JQKD82 (JADA82) dihydrochloride is a cell-permeable and selective KDM5 inhibitor. JQKD82 dihydrochloride increases H3K4me3 and can be used for the research of multiple myeloma[1].

JQKD 82 dihydrochloride is cell-permeable, selective inhibitor of lysine demethylase 5 (KDM5). JQKD 82 does not show activity toward other KDMs; and it has selectivity for KDM5A over other KDM5 isoforms. JQKD 82 causes hypermethylation of H3K4me3, downregulation of MYC targets and RNAPII phosphorylation; it suppresses multiple myeloma cell (MM.1S) growth (IC50 = 0.42 μmol/L). JQKD 82-treated tumors display an increase in H3K4me3 levels and results in a reduction of MYC immuno-staining in NSG mice.

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[1] Jun Qi, et al. Histone demethylase 5 inhibitors and uses thereof. WO2020033377A1.