2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease Immunology/Inflammation NF-κB Apoptosis Cytoskeleton
  3. Topoisomerase Reactive Oxygen Species (ROS) Apoptosis Microtubule/Tubulin
  4. DNA/TOP2A-IN-1

DNA/TOP2A-IN-1 是 DNA 和 TOP2A 的抑制剂。DNA/TOP2A-IN-1 选择性地与 TOP2A 结合，而非TOP2B，并与 DNA 和 TOP2A 相互作用形成稳定的 DM1-TOP2A-DNA 三元复合物。DNA/TOP2A-IN-1诱导 DNA 损伤，增加活性氧 (ROS)，并引发三阴性乳腺癌 (TNBC) 细胞凋亡 (apoptosis)。DNA/TOP2A-IN-1 破坏微管 (microtubule) 分布，诱导细胞周期停滞。DNA/TOP2A-IN-1 具有强大的抗增殖活性，并抑制细胞迁移。DNA/TOP2A-IN-1 可抑制肿瘤生长，可用于 TNBC 研究。

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DNA/TOP2A-IN-1

DNA/TOP2A-IN-1 Chemical Structure

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DNA/TOP2A-IN-1 相关抗体

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Topoisomerase Topo I Topo II

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

DNA/TOP2A-IN-1 is an inhibitor of DNA and TOP2A. DNA/TOP2A-IN-1 selectively binds to TOP2A, not TOP2B, and interacts with DNA and TOP2A to form a stable DM1-TOP2A-DNA ternary complex. DNA/TOP2A-IN-1 induces DNA damage, increases reactive oxygen species (ROS) and triggers apoptosis in triple-negative breast cancer (TNBC) cells. DNA/TOP2A-IN-1 disrupts microtubule distribution and induces cell cycle arrest. DNA/TOP2A-IN-1 shows strong antiproliferative activity and inhibits cell migration. DNA/TOP2A-IN-1 inhibits tumor growth and can be used for TNBC research[1].

IC50 & Target[1]

topoisomerase II alpha

 

体外研究
(In Vitro)

DNA/TOP2A-IN-1 (Compound DM1) 可以直接与 TOP2A 结合并破坏 DNA 二级结构[1]。
DNA/TOP2A-IN-1 (0-1.6 μM，24 小时) 可与 4T1 细胞中的 DNA 结合，促进三元 DM1-TOP2A-DNA 复合物的形成，并诱导细胞损伤[1]。
DM1 (10-100 μM，37 ℃，30 分钟) 通过抑制 TOP2A 介导的 DNA 松弛来抑制 TOP2A 活性[1]。
DNA/TOP2A-IN-1 (48 小时) 抑制多种癌细胞的增殖，IC50 分别为 1.12 μM (4T1)、2.53 μM (MDA-MB-231)、2.68 μM (MDA-MB-468)、5.02 μM (MCF-7)、3.80 μM (Hela)、3.44 μM (SiHa)、4.78 μM (PC9)、3.68 μM (A549)、2.7 μM (ID8)、2.69 μM (PANC1) 和 9.03 μM (BEAS-2B)[1]。
DNA/TOP2A-IN-1 剂量依赖性地抑制 4T1 和 MDA-MB-231 细胞活力 (0-4 μM，24-72 小时)、增殖 (0-3 μM，3 天) 和迁移 (0-12 μM，24 小时)[1]。
DNA/TOP2A-IN-1 (0-2.4 μM，24 小时) 在 4T1 和 MDA-MB-231 细胞中表现出微丝塌陷和解体，同时肌动蛋白和微管分布发生改变[1]。
DNA/TOP2A-IN-1 (0-7.2 μM，0-48 小时) 促进 4T1 细胞和 MDA-MB-231 细胞凋亡，并升高细胞内活性氧[1]。
DNA/TOP2A-IN-1 (0-12 μM，24 小时) 可诱导 4T1 和 MDA-MB-231 细胞周期停滞于 G2/M 期[1]。DNA/TOP2A-IN-1 (2 和 10 μM，6 天) 可显著抑制类器官中乳腺癌的生长[1]。

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

DNA/TOP2A-IN-1 相关抗体:

Immunofluorescence[1]

Cell Line: 4T1 and MDA-MB-231 cells
Concentration: 4T1: 1.2 μM, MDA-MB-231: 2.4 μM
Incubation Time: 24 h
Result: Induced collapsed and disintegrated microfilaments in 4T1 and MDA-MB-231 cells, along with altered actin and microtubule distribution (Confocal immunofluorescence).

Western Blot Analysis[1]

Cell Line: 4T1 cells
Concentration: 1.2, 1.4, 1.6 μM
Incubation Time: 24 h
Result: Markedly increased γ-H2AX expression.

Apoptosis Analysis[1]

Cell Line: 4T1 cells
Concentration: 1, 1.5, 2, 2.5, 3 μM
Incubation Time: 48 h for Annexin V-FITC staining; 0, 6, 12, 18, 24, 30 h for TUNEL staining; 0, 24, 30, 36, 42 h for WB
Result: Increased the percentage of apoptotic 4T1 cells from 15.12 % to 83.44 %.
Increased the TUNEL level over time.
Increased cleaved PARP and cleaved Caspase3, and decreased pro-Caspase9 protein level.

Cell Cycle Analysis[1]

Cell Line: 4T1 and MDA-MB-231 cells
Concentration: 4T1: 1, 1.5, 2, 2.5, 3 μM; MDA-MB-231: 4, 6, 8, 10, 12 μM
Incubation Time: 24 h
Result: Increased pcentage of cells in the G2/M phase and decreased the percentage of cells in the G0/G1 phase.
Downregulation of CDK4, CDK6, cyclin D, cyclin B and p-cdc2 (CDK1) protein expression level.
体内研究
(In Vivo)

DNA/TOP2A-IN-1 (Compound DM1) (20 和 30 mg/kg，腹腔注射，每两天一次，持续 14 天) 在 BALB/c 小鼠 4T1 肿瘤模型中显示出抗肿瘤作用[1]。

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

Animal Model: Female Balb/c mice (5 weeks old, 16-18 g) injected subcutaneously with 4T1 cells[1]
Dosage: 20 and 30 mg/kg
Administration: i.p., every two days for 14 days
Result: Inhibited tumor growth, with mean Tumor Growth Inhibition (TGI) of 80.76 % (30 mg/ kg) and 71.50 % (20 mg/kg).
Lowered the proportion of Ki67-positive tumor cells than in the solvent control group.
Revealed no significant drug-induced damage to the hearts, livers, spleens, lungs, and kidneys of the mice.
分子量

547.60

Formula

C32H29N5O4
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

DNA/TOP2A-IN-1 相关分类

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  • 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:

DNA/TOP2A-IN-1TopoisomeraseReactive Oxygen Species (ROS)ApoptosisMicrotubule/TubulinTumorbreast cancerTNBCcell cycle4T1MDA-MB-231organoidTOP2AantiproliferativeInhibitorinhibitorinhibit

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