2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease Immunology/Inflammation NF-κB Apoptosis
  3. Topoisomerase DNA/RNA Synthesis Reactive Oxygen Species (ROS) MDM-2/p53 Caspase
  4. Topoisomerase I-IN-18

Topoisomerase I-IN-18 是 Thiosemicarbazide (HY-Y0032) 的衍生物，是一种 Topoisomerase I 抑制剂。Topoisomerase I-IN-18 能够干扰 DNA 合成和转录。Topoisomerase I-IN-18 通过诱导 S 期细胞周期阻滞来抑制肿瘤细胞增殖。Topoisomerase I-IN-18 能够增强线粒体介导的细胞凋亡 (apoptosis)，表现为细胞迁移受到抑制和细胞内活性氧 (ROS) 水平升高。Topoisomerase I-IN-18 可增加 p53 蛋白表达、γH2AX 磷酸化、上调 Bax 表达、下调 Bcl-2 表达，并激活 caspase 级联反应。Topoisomerase I-IN-18可用于肺癌研究。

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Topoisomerase I-IN-18

Topoisomerase I-IN-18 Chemical Structure

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Topoisomerase I-IN-18 相关抗体

Top Publications Citing Use of Products

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Topoisomerase Topo I Topo II

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Topoisomerase I-IN-18, a derivative of Thiosemicarbazide (HY-Y0032), is a Topoisomerase I inhibitor. Topoisomerase I-IN-18 can disrupt DNA synthesis and transcription. Topoisomerase I-IN-18 inhibits tumor cell proliferation by inducing S-phase cell cycle arrest. Topoisomerase I-IN-18 can enhance mitochondria-mediated apoptosis, suppress cell migration, and increase intracellular Reactive Oxygen Species (ROS) levels. Topoisomerase I-IN-18 can increase p53 protein expression, γH2AX phosphorylation, upregulate Bax expression, downregulate Bcl-2 expression, and activate the caspase cascade. Topoisomerase I-IN-18 can be used for the study of lung cancer[1].

体外研究
(In Vitro)

Topoisomerase I-IN-18 (Compound 11d) 在所测试的癌细胞系中表现出不同的抗增殖活性，包括 MCF-7 (IC50 = 59.11 μM)、HepG-2 (IC50 = 67.63 μM)、SGC7901 (IC50 = 44.6 μM)、A549 (IC50 = 8.06 μM)，并且对正常 HK-2 细胞表现出最小的毒性[1]。
Topoisomerase I-IN-18 (1-10 μM) 通过剂量依赖性抑制作用有效阻断 Topo I 介导的超螺旋 DNA 松弛[1]。
Topoisomerase I-IN-18 (1-10 μM，48 小时) 作为 HY-178321（UNC10088）Topoisomerase I 抑制剂，可诱导 A549 细胞中出现剂量依赖性的 DNA 双链断裂[1]。
Topoisomerase I-IN-18 (1-10 μM，0-48 小时) 可有效抑制 A549 细胞的迁移和增殖，提示其具有潜在的抗转移特性[1]。
Topoisomerase I-IN-18 (4-16 μM，48 小时) 可剂量依赖性地在 A549 细胞中生成活性氧 (ROS) 并诱导细胞凋亡[1]。
Topoisomerase I-IN-18 (4-16 μM，24 小时) 在 A549 细胞中诱导剂量依赖性的 S 期阻滞，同时 G0/G1 和 G2/M 细胞群减少，并显著增加 γ-H2AX 磷酸化，调节关键凋亡相关蛋白的表达，表现为 p53、Bax、caspase-3 和 caspase-9 的上调以及 Bcl-2 的下调[1]。
Topoisomerase I-IN-18被鉴定为P-糖蛋白 (P-gp) 底物，并可能抑制细胞色素P450酶 (CYP1A2、CYP2C19、CYP2D6和CYP3A4)[1]。

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

Topoisomerase I-IN-18 相关抗体:

Cell Migration Assay [1]

Cell Line: A549 cells
Concentration: 1 μM, 5 μM, 10 μM
Incubation Time: 0 h, 24 h, 48 h
Result: Significantly inhibited wound closure at 10 μM, while even at 2.5 μM, A549 cell migration capacity was considerably reduced.
Wound closure percentage in treated cells decreased dose-dependently with increasing concentration (from 46.25 % at 2.5 μM to 21.36 % at 10 μM).

Cell Cycle Analysis[1]

Cell Line: A549 cells
Concentration: 4 μM, 8 μM, 16 μM
Incubation Time: 24 h
Result: Dose-dependent S-phase blockade, with a decrease in the G0/G1 and G2/M phase ratios.

Western Blot Analysis[1]

Cell Line: A549 cells
Concentration: 0 μM, 4 μM, 8 μM, 16 μM
Incubation Time: 24 h
Result: Increased γ-H2AX phosphorylation levels in a dose-dependent manner, upregulated the expression of p53, Bax, caspase-3, and caspase-9, and downregulated Bcl-2 expression in A549 cells.
分子量

431.61

Formula

C23H34FN5S
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

Topoisomerase I-IN-18 相关分类

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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:

Topoisomerase I-IN-18TopoisomeraseDNA/RNA SynthesisReactive Oxygen Species (ROS)MDM-2/p53CaspaseAnti-cancer agentsApoptosisCell cycleMatrine derivativesTopoisomerase I inhibitorsInhibitorinhibitorinhibit

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目录号：
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