2. Epigenetics
  3. Histone Methyltransferase
  4. EZM8266

EZM8266 是一种具有口服活性和选择性的 G9a (EHMT2) 组蛋白甲基转移酶抑制剂，对人源 EHMT2 的 IC50 为 1 pM。EZM8266 可降低免疫刺激基因及内源性逆转录病毒元件启动子区域的抑制性 H3K9me2 修饰标记。EZM8266 可抑制癌细胞的集落形成、迁移及侵袭能力。EZM8266 可增强癌细胞中的 IFN-γ 应答，提高 MHC I 类分子的表达水平，并增强 CXCL10 介导的 T 细胞募集作用。EZM8266 可用于肝细胞癌的相关研究。

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EZM8266

EZM8266 Chemical Structure

CAS No. : 2140164-84-5

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规格 价格 是否有货
5 mg ￥1160
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10 mg ￥1840
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25 mg ￥3280
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50 mg ￥5200
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EZM8266 相关抗体

Top Publications Citing Use of Products

查看 Histone Methyltransferase 亚型特异性产品:

查看所有亚型
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

EZM8266 is an orally active and selective G9a (EHMT2) histone methyltransferase inhibitor with a human EHMT2 IC50 of 1 pM. EZM8266 reduces repressive H3K9me2 marks at immune-stimulatory gene and endogenous retroviral element promoters. EZM8266 reduces colony formation, migration, and invasion of cancer cells. EZM8266 enhances IFN-γ response, increases MHC class I expression, and enhances CXCL10-mediated T cell recruitment in cancer cells. EZM8266 can be used for the research of hepatocellular carcinoma[1][2].

IC50 & Target[1]

G9a

1 pM (IC50)

体外研究
(In Vitro)

EZM8266 (Compound 5R) (0.5-10 μM；~15 天) 可强效抑制人 PLC/PRF/5 HCC 细胞的集落形成[1]。
EZM8266 (0.5-10 μM；3 周) 呈剂量依赖性抑制人 PLC/PRF/5 HCC 细胞的锚定非依赖性生长[1]。
EZM8266 (1-5 μM；72 小时) 可剂量依赖性地抑制人源 HuH7 肝癌细胞的迁移[1]。
EZM8266 (1-5 μM；72 小时) 呈剂量依赖性抑制人源 HuH7 肝癌 (HCC) 细胞的侵袭[1]。
EZM8266 (5 μM；48 小时) 可在人 PLC/PRF/5 肝癌 (HCC) 细胞中诱导广泛的转录重编程，上调包括固有免疫应答、干扰素信号通路和双链 RNA (dsRNA) 加工在内的免疫相关通路[1]。
EZM8266 (5 μM；72 小时) 单独使用或与 IFN-γ 联用时，可增强小鼠 PM299L 肝癌细胞中 IFN-γ 介导的免疫相关基因 (包括趋化因子、MHC I 类组分及干扰素应答基因) 的上调表达[1]。
EZM8266 (5 mM；72 小时) 与 IFN-γ 联用时，可协同显著提高小鼠 PM299L 和人 HuH7 肝癌细胞中 CXCL10 的分泌水平[1]。
EZM8266 (5 mM；72 小时) 单独使用或与 IFN-γ 联合使用时，可增强 IFN-γ 介导的小鼠 PM299L 细胞和人 HuH7 肝癌 (HCC) 细胞表面 MHC I 类分子表达的上调[1]。
EZM8266 (48 h) 可诱导小鼠和人 HCC 细胞内的双链 RNA 显著累积[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

EZM8266 相关抗体:

Cell Invasion Assay[1]

Cell Line: human HuH7 HCC cells
Concentration: 1 μM; 2.5 μM; 5 μM
Incubation Time: 24 h
Result: Significantly reduced cell invasion in a dose-dependent manner, with ~60%, ~80%, and ~90% reductions at 1, 2.5, and 5 μM respectively, compared to control.

Real Time qPCR[1]

Cell Line: murine PM299L HCC cells
Concentration: 5 μM
Incubation Time: 72 h
Result: Upregulated expression of Cxcl9, Cxcl10, B2m, Hla-a, Nlrc5, Mda5, Stat1, Rigi, Casp1, Lgals3bp, Tap1, and Irgm2 when used alone.
Produced a synergistic increase in expression of all these genes when combined with IFN-γ compared to either treatment alone.

ELISA Assay[1]

Cell Line: murine PM299L and human HuH7 HCC cells
Concentration: 5 mM
Incubation Time: 72 h
Result: Slightly increased CXCL10 secretion when used alone, while IFN-γ alone induced a moderate increase.
Produced a synergistic, significant increase in CXCL10 secretion when combined with IFN-γ compared to either treatment alone in both PM299L and HuH7 cells.
体内研究
(In Vivo)

EZM8266 (Compound 5R) (300 mg/kg；口服；每日) 在原位小鼠肝癌模型中可显著抑制肿瘤生长，并增加瘤内 CD8+和 CD4+ T 细胞浸润[1]。
EZM8266 (300 mg/kg；口服；每周 5 天；持续 4 周) 单药治疗可显著降低原位小鼠肝癌模型的肿瘤负荷与发病率，与抗 PD-1 联合用药则进一步增强抗肿瘤疗效、使血清肝酶水平恢复正常，并增加肿瘤内 CD8+和 CD4+ T 细胞浸润[1]。
EZM8266 (300 mg/kg；口服；每周 5 天；持续 4 周) 单药治疗可显著降低 MYC/β-catenin 驱动的小鼠 HCC 模型中的肿瘤负荷，且与抗 PD1 联合用药可增强抗肿瘤疗效，并将肿瘤微环境重塑为免疫抑制性更低的状态[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J (male, 6-8 weeks old, orthotopic implantation of PM299L murine HCC tumor fragments)[1]
Dosage: 300 mg/kg
Administration: p.o.; daily
Result: Significantly reduced tumor growth compared to vehicle controls.
Significantly lowered final tumor weights compared to vehicle controls.
Increased tumor-infiltrating CD8+ T cell counts to a mean of ~100 cells/mm2 (from vehicle mean ~30 cells/mm2).
Increased CD4+ T cell counts to a mean of ~100 cells/mm2 (from vehicle mean ~30 cells/mm2).
Animal Model: C57BL/6J (male, 6-8 weeks old, intrahepatic injection of PM299L murine HCC cells)[1]
Dosage: 300 mg/kg; 300 mg/kg plus 100 μg/mouse anti-PD1
Administration: p.o.; 5 days per week; 4 weeks
Result: Reduced liver index (tumor burden) from a vehicle mean of ~18% to ~7% with monotherapy.
Reduced tumor incidence from 100% to 80% with monotherapy.
Further reduced liver index to ~3% with combination therapy.
Further reduced tumor incidence to 50% with combination therapy.
Reduced serum alanine transaminase (ALT), aspartate transaminase (AST), and lactate dehydrogenase (LDH) levels to levels comparable to age-matched normal mice.
Increased tumor-infiltrating CD8+ T cell counts to a mean of ~6000 cells/mm2 with monotherapy, and to ~8000 cells/mm2 with combination therapy (from vehicle mean ~1000 cells/mm2).
Increased CD4+ T cell counts to a mean of ~15000 cells/mm2 with combination therapy (from vehicle mean ~5000 cells/mm2).
Reduced tumor area from a vehicle mean of ~80 μm2 to ~20 μm2 with monotherapy, and to ~5 μm2 with combination therapy.
Animal Model: C57BL/6J (male, 4 weeks old, hydrodynamic tail vein injection of MYC/CTNNB1-Δ90 transposon vectors)[1]
Dosage: 300 mg/kg; 300 mg/kg plus 100 μg/mouse anti-PD1
Administration: p.o.; 5 days per week; 4 weeks
Result: Elicited a significant antitumor response with monotherapy.
Resulted in a pronounced reduction in tumor burden with combination therapy.
Increased infiltration of CD8+ and CD4+ T lymphocytes with combination therapy.
Decreased CD4+:CD8+ ratio with combination therapy.
Reduced regulatory T cells with combination therapy.
Preserved effector memory subsets without overt T cell exhaustion with combination therapy.
分子量

373.45

Formula

C19H27N5O3
CAS 号
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.
纯度 & 产品资料
参考文献

EZM8266 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

EZM82662140164-84-5EZM 8266EZM-8266Histone MethyltransferasePLC/PRF/5 HCC cellsH3K9me2CD8+ T cellG9ahepatocellular carcinomaCD4+ T cellPM299L HCC cellsHuH7 HCC cellsEHMT2histone methyltransferaseInhibitorinhibitorinhibit

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