JQKD82

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

JQKD82 是 KDM5 的选择性抑制剂，可增加 H3K4me3。 JQKD82可用于有关多发性骨髓瘤治疗的研究。

JQKD82 is a selective inhibitor of KDM5 and increases H3K4me3. JQKD82 can be used in studies about the treatment of multiple myeloma.(In Vitro):In MM.1S and MOLP-8 cells, JQKD82 (1 μM) induces G1 cell cycle arrest. JQKD82 (0.3 μM) increases global H3K4me3 levels in MM.1S cells. JQKD82 (0.1-10 μM) inhibits the growth of MM.1S cells in a dose- and time-dependent manner (IC50 = 0.42 μM).(In Vivo):In female NSG mice bearing MOLP-8 TurboGFP-Luc cells, JQKD82 (50 and 75 mg/kg; i.p.) significantly reduces tumor burden. JQKD82 increases the level of H3K4me3 and significantly reduces MYC immuno-staining in vivo.

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.

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.

JADA82 | PCK82

Chromatin/Epigenetic

Histone Demethylase

L. donovani

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2410512-38-6

500.63

C27H40N4O5

>98% (HPLC)

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O=C(OC1=CC=C(OC(C)C)C=C1OC(C)C)C=2C=CN=C(C2)CNCC(=O)N(CC)CCN(C)C

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(-20℃)

With Ice Pack

≥ 2 years