产品
编 号：F238629
分子式：C30H38N8O2
分子量：542.68
分子式：C30H38N8O2
分子量：542.68
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 1913252-04-6
产品详情
生物活性：
JQEZ5 is a potent and selective EZH2 lysine methyltransferase inhibitor. JQEZ5 SAM-competitively inhibits polycomb repressive complex 2 (PRC2) with an IC50 of 80 nM. JQEZ5 has anti-tumor effects.
体内研究：
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.
体外研究：
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.
JQEZ5 is a potent and selective EZH2 lysine methyltransferase inhibitor. JQEZ5 SAM-competitively inhibits polycomb repressive complex 2 (PRC2) with an IC50 of 80 nM. JQEZ5 has anti-tumor effects.
体内研究：
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.
体外研究：
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.
产品资料
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