2. Cell Cycle/DNA Damage Cytoskeleton Apoptosis NF-κB Metabolic Enzyme/Protease Immunology/Inflammation
  3. Microtubule/Tubulin Apoptosis Reactive Oxygen Species (ROS)
  4. Tubulin-IN-53

Tubulin-IN-53 是一种强效的微管蛋白 (Tubulin) 抑制剂，其 IC50 为 6.06 μM。Tubulin-IN-53 通过靶向微管蛋白的秋水仙碱结合位点来抑制微管蛋白的聚合，破坏微管网络。Tubulin-IN-53 诱导 MCF-7 细胞周期停滞于 G2/M 期并导致细胞凋亡 (apoptosis)，同时抑制细胞迁移，并伴随线粒体膜电位降低和活性氧 (ROS) 积累增加。Tubulin-IN-53 还能破坏人脐静脉内皮细胞的血管生成。Tubulin-IN-53 可用于乳腺癌和肺癌等癌症研究。

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Tubulin-IN-53

Tubulin-IN-53 Chemical Structure

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Tubulin-IN-53 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Tubulin-IN-53 is a potent Tubulin inhibitor with an IC50 of 6.06 μM. Tubulin-IN-53 inhibits the polymerization of tubulin by targeting the colchicine binding site of tubulin and destroys the microtubule network. Tubulin-IN-53 induces MCF-7 cell cycle arrest in the G2/M phase and apoptosis, and inhibits cell migration accompanied by the decrease of mitochondrial membrane potential and increase the accumulation of ROS. Tubulin-IN-53 destroys the angiogenesis of human umbilical vein endothelial cells.Tubulin-IN-53 can used for the study of cancers such as breast cancer and lung cancer[1].

体外研究
(In Vitro)

Tubulin-IN-53 (Compound A7) (72 h) 在多种癌细胞中表现出抗增殖活性，对 PC-3、MCF-7、MDA-MB-231、A549、HT-29 和 A549/TxR 细胞的 IC50 分别为 6、4、5、6、4 和 10 nM，对正常细胞具有轻度细胞毒性，对 L02 和 MCF-10A 细胞的 CC50 分别为 112 和 220 nM[1]。
Tubulin-IN-53 (5-20 nM, 14 d) 持续抑制 MCF-7 细胞集落形成[1]。
Tubulin-IN-53 (5-20 nM, 6 h) 以剂量依赖性方式抑制 EBI 与 β-微管蛋白加合物的形成，并且可完全分解 MCF-7 细胞中的微管网络[1]。
Tubulin-IN-53 (5-20 nM, 24 h) 可诱导 MCF-7 细胞周期停滞于 G2/M 期并引发细胞凋亡，同时显著升高细胞内 ROS 水平[1]。
Tubulin-IN-53 (2.5-10 nM, 24 h) 可抑制 A549 细胞迁移，并有效抑制内皮细胞中血管网络的形成[1]。

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

Tubulin-IN-53 相关抗体:

Apoptosis Analysis[1]

Cell Line: MCF-7 cells
Concentration: 5, 10 and 20 nM
Incubation Time: 24 h
Result: Significantly increased apoptosis rate.

Cell Cycle Analysis[1]

Cell Line: MCF-7 cells
Concentration: 5, 10 and 20 nM
Incubation Time: 24 h
Result: Increased the G2/M phase ratio of MCF-7 cells from 18.7% to 76.1%.

Western Blot Analysis[1]

Cell Line: MCF-7 cells
Concentration: 5, 10 and 20 nM
Incubation Time: 24 h
Result: Upregulated Cyclin B1 expression and reduced Cdc2 phosphorylation (Y15) levels.
Downregulates the anti-apoptotic protein Bcl-2 and upregulates the pro-apoptotic protein Bax.
Increased cleaved PARP and cleaved caspase-3 levels.

Cell Migration Assay [1]

Cell Line: A549 cells
Concentration: 2.5, 5 and 10 nM
Incubation Time: 24 h
Result: Significantly reduced the number of A549 cells penetrating the membrane.
Significantly inhibited the migration ability of A549 cells.
分子量

401.80

Formula

C20H16ClNO6
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

Tubulin-IN-53 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:

Tubulin-IN-53Microtubule/TubulinApoptosisReactive Oxygen Species (ROS)TubulinDeoxypodophyllotoxinAntiproliferativeAntitumorInhibitorinhibitorinhibit

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