1. Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease Immunology/Inflammation NF-κB Apoptosis
  2. Nuclear Hormone Receptor 4A/NR4A Reactive Oxygen Species (ROS) Glutathione Peroxidase Ferroptosis Transferrin Receptor
  3. DIM-3,5-Cl2

DIM-3,5-Cl2 是一种反向 NR4A1/NR4A2 激动剂。DIM-3,5-Cl2 可下调由 NR4A1/NR4A2 调控的促癌反应/基因产物。DIM-3,5-Cl2 可诱导活性氧 (ROS)、丙二醛和脂质过氧化物的生成,并伴有 GPX4 和 SLC7A11 表达降低以及 CD71 表达上调。DIM-3,5-Cl2 可诱导铁死亡 (ferroptosis)。DIM 可用于三阴性乳腺癌的研究。

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DIM-3,5-Cl2

DIM-3,5-Cl2 Chemical Structure

CAS No. : 2595179-74-9

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

DIM-3,5-Cl2 is an inverse NR4A1/NR4A2 agonist. DIM-3,5-Cl2 can downregulate the pro-oncogenic responses/gene products regulated by NR4A1/NR4A2. DIM-3,5-Cl2 can induce ROS, malondialdehyde, and lipoperoxide formation, and this was accompanied by decreased expression of GPX4 and SLC7A11 and induction of CD71. DIM-3,5-Cl2 can induce ferroptosis. DIM-3,5-Cl2 can be used for the study of triple-negative breast cancer[1].

IC50 & Target

Nur77/NR4A1

 

Nurr1/NR4A2

 

体外研究
(In Vitro)

DIM-3,5-Cl2 (2.5-15 μM,24 小时) 呈剂量依赖性地降低三种乳腺癌细胞的存活率[1]
DIM-3,5-Cl2 (7-15 μM,24 小时) 通过调节乳腺癌细胞中的 NR4A1/2 通路诱导细胞凋亡并下调多种癌基因[1]
DIM-3,5-Cl2 (10-12 μM,4-24 小时) 显著诱导乳腺癌细胞系中活性氧 (ROS) 的产生,使用 H2DCFDA 染料 (HY-D0940) 检测;并且诱导 MDA-MB-231、MDA-MB-468 和 4T1 细胞中脂质过氧化,使用 BODIPY 581/591 C11 探针 (HY-D1301) 检测[1]
DIM-3,5-Cl2 (12 μM,16 小时) 显著增加 MDA-MB-231、MDA-MB-468 和 4T1 细胞中的 MDA 水平[1]
DIM-3,5-Cl2 (7-15 μM,24 小时) 下调 MDA-MB-231、MDA-MB-468 和 4T1 细胞中 GPX4 和 SLC7A11 蛋白的表达,而 CD71 的表达在低浓度 (10 μM 以内) 下调,在高浓度 (12-15 μM) 下调[1]
DIM-3,5-Cl2 (7-10 μM,1-6 小时) 在 6 小时内诱导 MDA-MB-231 细胞中 CD71 蛋白表达和 CD71 mRNA 水平升高[1]
DIM-3,5-Cl2 (15 μM) 可诱导 PDX 来源的类器官 (PDxO) 中 CD71 蛋白的表达[1]
DIM-3,5-Cl2 (10-12 μM,4-24 小时) 可降低 MDA-MB-231 细胞中 NR4A1 和 NR4A2 蛋白的水平,同时诱导 Sp1 和 Sp4 蛋白的表达[1]
DIM-3,5-Cl2 (10-12 μM,6 小时) 可诱导 MDA-MB-231、MDA-MB-468 和 4T1 细胞中 CD71 启动子的活性[1]
DIM-3,5-Cl2 (10-12 小时,24 小时) 可诱导 MDA-MB-231、MDA-MB-468 和 4T1 细胞中荧光素酶的活性,但在高浓度下,它会部分抑制荧光素酶的活性[1]

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

Cell Proliferation Assay[1]

Cell Line: MDA-MB-231 cells, MDA-MB-468 cells, 4T1 cells
Concentration: 2.5 μM, 5 μM, 7 μM, 10 μM, 12 μM, 15 μM
Incubation Time: 24 h
Result: Dose-dependent reduced in the survival rate of three types of breast cancer cells.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells, MDA-MB-468 cells, 4T1 cells
Concentration: 7 μM, 10 μM, 12 μM, 15 μM
Incubation Time: 24 h
Result: Induced the expression of cleaved PARP and cleaved caspase-3, and reduced the protein levels of BCL-2, PARP, caspase-3, EGFR, β1-integrin, and c-Myc.
分子量

391.29

Formula

C23H16Cl2N2

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
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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.

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