JQKD82 (JADA82) trihydrochloride is a cell-permeable and selective KDM5 inhibitor. JQKD82 trihydrochloride increases H3K4me3 and can be used for the research of multiple myeloma[1].
JQKD82 (0.3 μM; 24 hours) trihydrochloride causes an increase in the global H3K4me3 level of MM.1S cells[1].JQKD82 (0.1-10 μM; day 1-day 5) trihydrochloride inhibits the growth of MM.1S cells in a dose- and time-dependent manner. JQKD82 trihydrochloride is potent at eliciting growth suppression in MM.1S cells (IC50=0.42 μM)[1].JQKD82 (1 μM; 24 hours) trihydrochloride induces G1 cell-cycle arrest by 48 hours in MM.1S and MOLP-8 cells[1].
JQKD82 (50-75 mg/kg; i.p.; twice a day for 3 weeks) trihydrochloride has anti-multiple myeloma activity[1].JQKD82 trihydrochloride displays an increase in H3K4me3 levels and results in a dramatic reduction of MYC immuno-staining in vivo[1].
[1]. Jun Qi, et al. Histone demethylase 5 inhibitors and uses thereof. WO2020033377A1.