2. Epigenetics GPCR/G Protein Immunology/Inflammation NF-κB Metabolic Enzyme/Protease Autophagy Apoptosis
  3. Histone Methyltransferase GLP Receptor Reactive Oxygen Species (ROS) Autophagy Apoptosis
  4. G9a-IN-4

G9a-IN-4 是一种 G9a 特异性抑制剂 (IC50 = 32 nM)。G9a-IN-4 对其他测试的赖氨酸/精氨酸甲基转移酶表现出很高的选择性。G9a-IN-4 展示出较高的酶活性，并且对所有测试的癌细胞均表现出更强的抗增殖作用。G9a-IN-4 显著抑制了 H3K9me2 的水平。G9a-IN-4 通过诱导 ROS 的产生来触发自噬 (autophagy)，从而导致 CT26 结肠癌细胞凋亡 (apoptosis) 和 G0/G1 期细胞周期阻滞。G9a-IN-4 可用于结肠癌的研究。

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G9a-IN-4

G9a-IN-4 Chemical Structure

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G9a-IN-4 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 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

G9a-IN-4 is a G9a inhibitor with high selectivity (IC50 = 32 nM). G9a-IN-4 shows high selectivity against the other tested lysine/arginine methyltransferases. G9a-IN-4 exhibits high enzymatic activity against G9a and more potent antiproliferative effects against all tested cancer cells. G9a-IN-4 significantly suppresses the H3K9me2 level. G9a-IN-4 triggers autophagy by inducing the production of ROS, thus leading to cell apoptosis and cell cycle arrest at G0/G1 in CT26 colon cells. G9a-IN-4 can be used for the study of colon cancer[1].

体外研究
(In Vitro)

G9a-IN-4 (Compound 31) 是一种特异性 G9a/GLP 抑制剂 (IC50 = 0.2 nM；IC50 = 0.43 nM) ，对 AlphaLISA 中测试的其他表观遗传靶点也具有高选择性[1]。
G9a-IN-4 对所有测试的癌细胞均表现出更强的抑制作用，包括血液肿瘤细胞：RPMI8226 (IC50 = 0.85 μM) 、MV-4-11 (IC50 = 0.49 μM) 、Jeko-1 (IC50 = 0.7 μM) 、Molt4 (IC50 = 1.34 μM)，以及实体瘤细胞：HeLa (IC50 = 1.55 μM) 、U2OS (IC50 = 3 μM) 、CT26 (IC50 = 3.31 μM)[1]。
G9a-IN-4 (1.25-2.5 μM，72 h) 以剂量依赖的方式显著降低 CT26 细胞中 H3K9 的二甲基化水平[1]。
G9a-IN-4 (2.5-5 μM，48 h) 以剂量依赖的方式显著诱导 CT26 细胞中活性氧 (ROS) 的积累[1]。
G9a-IN-4 (2.5-10 μM，12 h) 在 10 μM 浓度下显著降低 LC3-I 的表达，并在所有测试浓度下均显著提高 LC3-II 的水平，从而以剂量依赖的方式增加 LC3-II 与 LC3-I 的比值，有效诱导 CT26 细胞的自噬[1]。
G9a-IN-4 (2.5-10 μM，24 小时) 可剂量依赖性地将诱导 CT26 细胞凋亡比例从 5.48 % 提高至 91.37 %[1]。
G9a-IN-4 (2.5-5 μM，24 小时) 可诱导 CT26 细胞发生 G0/G1 期阻滞[1]。

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

G9a-IN-4 相关抗体:

Western Blot Analysis[1]

Cell Line: CT26 cells
Concentration: 1.25 μM, 2.5 μM
Incubation Time: 72 h
Result: Induced a marked reduction in the dimethylation of H3K9 in CT26 cells in a dose-dependent manner.

Cell Autophagy Assay[1]

Cell Line: CT26 cells
Concentration: 2.5 μM, 5 μM, 10 μM
Incubation Time: 72 h
Result: Significantly decreased LC3-I expression at 10 μM and increased the LC3-II level at all tested concentrations, thus leading to an increased ratio of LC3-II to LC3-I in a dose-dependent manner.
Effectively induced autophagy in CT26 cells.

Cell Cycle Analysis[1]

Cell Line: CT26 cells
Concentration: 2.5 μM, 5 μM
Incubation Time: 24 h
Result: Induced a marked reduction in the dimethylation of H3K9 in CT26 cells in a dose-dependent manner.
体内研究
(In Vivo)

G9a-IN-4 (10 mg/kg，腹腔注射，每两天一次，持续两周) 能有效抑制结肠癌小鼠模型中的肿瘤，而不会造成明显的体重减轻或死亡[1]。

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

Animal Model: CT26 cells (5 × 105 cells/mouse) were subcutaneously implanted into the right armpit of female BALB/c mice (6 weeks)[1].
Dosage: 10 mg/kg
Administration: I.p., once every two days for two weeks
Result: Significantly suppressed tumor growth with a 45.1 % (TGI) reduction in tumor weight.
Exhibited a negligible impact on the body weight of mice without mortality during the 14-day treatment.
分子量

616.79

Formula

C35H48N6O4
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

G9a-IN-4 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

G9a-IN-4Histone MethyltransferaseGLP ReceptorReactive Oxygen Species (ROS)AutophagyApoptosisAntitumorG9a inhibitorLysine methyltransferaseStructural optimizationTetrahydroisoquinolineInhibitorinhibitorinhibit

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