| Description |
JQKD82 (JADA82) is a cell-permeable and selective KDM5 inhibitor. JQKD82 increases H3K4me3 and can be used for the research of multiple myeloma[1].
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| Related Catalog |
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| In Vitro |
JQKD82 (0.3 μM; 24 hours) causes an increase in the global H3K4me3 level of MM.1S cells[1]. JQKD82 (0.1-10 μM; day 1-day 5) inhibits the growth of MM.1S cells in a dose- and time-dependent manner. JQKD82 is potent at eliciting growth suppression in MM.1S cells (IC50=0.42 μM)[1]. JQKD82 (1 μM; 24 hours) induces G1 cell-cycle arrest by 48 hours in MM.1S and MOLP-8 cells[1].
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| In Vivo |
JQKD82 (50-75 mg/kg; i.p.; twice a day for 3 weeks) has anti-multiple myeloma activity[1]. JQKD82 displayed an increase in H3K4me3 levels and results in a dramatic reduction of MYC immuno-staining in vivo[1]. Animal Model: Six-week-old female NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ (NSG) mice (bearing MOLP-8 TurboGFP-Luc cells)[1] Dosage: 50 mg/kg, 75 mg/kg Administration: i.p.; twice a day for 3 weeks Result: Significantly reduced tumor burden.
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| References |
[1]. Jun Qi, et al. Histone demethylase 5 inhibitors and uses thereof. WO2020033377A1.
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