
JQEZ-5
CAS No. 1913252-04-6
JQEZ-5 ( EZ-005 | EZ005 | JQEZ5 )
产品货号. M12997 CAS No. 1913252-04-6
一种新型有效、选择性、SAM 竞争性 EZH2 抑制剂,IC50 为 80 nM(抑制 PRC2 的酶功能)。
纯度: >98% (HPLC)






规格 | 价格/人民币 | 库存 | 数量 |
5MG | ¥721 | 有现货 |
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10MG | ¥1037 | 有现货 |
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25MG | ¥2122 | 有现货 |
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50MG | ¥3969 | 有现货 |
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100MG | ¥5792 | 有现货 |
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200MG | 获取报价 | 有现货 |
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500MG | 获取报价 | 有现货 |
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1G | 获取报价 | 有现货 |
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生物学信息
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产品名称JQEZ-5
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注意事项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
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产品简述一种新型有效、选择性、SAM 竞争性 EZH2 抑制剂,IC50 为 80 nM(抑制 PRC2 的酶功能)。
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产品描述A novel potent, selective, SAM-competitive EZH2 inhibitor with IC50 of 80 nM (inhibition of enzymatic function of PRC2); demonstrates acutely reduced level of H3K27me3 without affecting mono- and di-methylation, suppresses the proliferation of EZH2-overexpression H661 and H522 cell lines, more effectively than GSK-126 and GSK-343; promotes the regression of EZH2-driven tumors in vivo.
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体外实验JQEZ5 inhibits enzymatic functionality of PRC2 with a biochemical IC50 of 80nM. JQEZ5 exhibits S-adenosyl methionine (SAM)-competitive inhibition of PRC2.H661 cells treated with increasing concentrations of JQEZ5 demonstrate acutely reduced levels of H3K27me3 without affecting H3K27 mono- or di-methylation. JQEZ5 suppresses the proliferation of EZH2-overexpressing H661 and H522 cells after treatment for 4 days without affecting the proliferation of cell lines that were deemed insensitive to EZH2 knockdown.
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体内实验JQEZ5 (75 mg/kg; intraperitoneal injection; daily; for 3 weeks) treatment exhibits rapid and pronounced tumor regression over the three week treatment course. And H3K27me3 levels are largely reduced with treatment further confirming the on-target effect of JQEZ5 in mice.
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同义词EZ-005 | EZ005 | JQEZ5
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通路Chromatin/Epigenetic
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靶点HMTase
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受体HMTase
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研究领域——
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适应症——
化学信息
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CAS Number1913252-04-6
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分子量542.688
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分子式C30H38N8O2
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纯度>98% (HPLC)
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溶解度DMSO : 25 mg/mL 46.07 mM;H2O : < 0.1 mg/mL
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SMILESCC(C)N1N=CC2=C(C=C(N=C12)C3=CC=C(N4CCN(CC4)C)N=C3)C(NCC5=C(CCC)C=C(C)NC5=O)=O
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化学全称N-[(6-methyl-2-oxo-4-propyl-1H-pyridin-3-yl)methyl]-6-[6-(4-methylpiperazin-1-yl)pyridin-3-yl]-1-propan-2-ylpyrazolo[3,4-b]pyridine-4-carboxamide
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
1. Zhang H, et al. Cancer Discov. 2016 Sep;6(9):1006-21.
2. Frankel AE, et al. Cancer Discov. 2016 Sep;6(9):949-52.