JQKD82(Synonyms: JADA82; PCK82)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

JQKD82 (Synonyms: JADA82; PCK82)

JQKD82 (JADA82) 是一种细胞通透性和选择性 KDM5 抑制剂。JQKD82 增加 H3K4me3，可用于多发性骨髓瘤的研究。

JQKD82(Synonyms: JADA82; PCK82)

JQKD82 Chemical Structure

CAS No. : 2410512-38-6

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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[1].

体外研究
(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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

500.63

Formula

C27H40N4O5
CAS 号

2410512-38-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

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

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