产品
编 号:F741552
分子式:C27H40N4O5
分子量:500.63
产品类型
结构图
CAS No: 2410512-38-6
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产品详情
生物活性:
JQKD82 (JADA82) is a cell-permeable and selective KDM5 inhibitor. JQKD82 increases H3K4me3 and can be used for the research of multiple myeloma.
体内研究:
JQKD82 (50-75 mg/kg; i.p.; twice a day for 3 weeks) has anti-multiple myeloma activity.JQKD82 displays an increase in H3K4me3 levels and results in a dramatic reduction of MYC immuno-staining in vivo.Animal Model:Six-week-old female NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ (NSG) mice (bearing MOLP-8 TurboGFP-Luc cells)
Dosage:50 mg/kg, 75 mg/kg
Administration:i.p.; twice a day for 3 weeks
Result:Significantly reduced tumor burden.
体外研究:
JQKD82 (0.3 μM; 24 hours) causes an increase in the global H3K4me3 level of MM.1S cells.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).JQKD82 (1 μM; 24 hours) induces G1 cell-cycle arrest by 48 hours in MM.1S and MOLP-8 cells.