2. Cell Cycle/DNA Damage Cytoskeleton Apoptosis
  3. Microtubule/Tubulin Caspase Apoptosis
  4. Tubulin polymerization-IN-89

Tubulin polymerization-IN-89 是一种微管蛋白聚合 (Tubulin polymerization) 抑制剂。Tubulin polymerization-IN-89 可结合微管蛋白异二聚体上的秋水仙碱结合位点，破坏微管蛋白聚合与微管形成。Tubulin polymerization-IN-89 可诱导黑色素瘤细胞发生凋亡 (apoptosis)，并阻滞细胞周期于 G2/M 期。Tubulin polymerization-IN-89 可用于转移性黑色素瘤的相关研究。

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Tubulin polymerization-IN-89

Tubulin polymerization-IN-89 Chemical Structure

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Tubulin polymerization-IN-89 相关抗体

Top Publications Citing Use of Products

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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

Tubulin polymerization-IN-89 is a tubulin polymerization inhibitor. Tubulin polymerization-IN-89 binds to the colchicine-binding site on tubulin heterodimers, disrupting tubulin polymerization and microtubule formation. Tubulin polymerization-IN-89 induces apoptosis in melanoma cells and arrests the cell cycle at the G2/M phase. Tubulin polymerization-IN-89 can be used in studies related to metastatic melanoma[1].

体外研究
(In Vitro)

Tubulin polymerization-IN-89 (compound 9d) (100 nM; 24 h) 可破坏微管网络，诱导 G2/M 期细胞周期阻滞，并通过激活 cleaved caspase-3 和 cleaved PARP 触发 A375 细胞凋亡[1]。
Tubulin polymerization-IN-89 在多种黑色素瘤细胞系中表现出强细胞毒性，其 GI50 值如下：A375 (15.4 nM)、RPMI-7951 (17.0 nM)、A2058 (13.8 nM) 以及紫杉醇耐药株 A375/TxR (24.7 nM)[1]。
Tubulin polymerization-IN-89 (20-40 nM; 24 h) 抑制 A375/TxR 细胞的迁移与侵袭[1]。
Tubulin polymerization-IN-89 (25-100 nM) 可完全消除 A375 细胞的集落形成[1]。

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

Tubulin polymerization-IN-89 相关抗体:

Cell Cycle Analysis[1]

Cell Line: A375 melanoma cells
Concentration: 100 nM
Incubation Time: 24 h
Result: Induced G2/M cell cycle arrest, with 80% of cells in G2/M phase.

Cell Migration Assay[1]

Cell Line: paclitaxel-resistant A375/TxR cells
Concentration: 20, 40 nM
Incubation Time: 24 h
Result: Inhibited cell migration by 86% at 40 nM.
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 Tmax Cmax AUClast AUCinf MRT0-inf
Mice[1] 10 mg/kg i.p. 1.49 h 8.34 min 316 ng/mL 263 ng·h/mL 271 ng·h/mL 1.37 h
体内研究
(In Vivo)

Tubulin polymerization-IN-89 (10-15 mg/kg；腹腔注射；每周 3 次；17 天) 在紫杉醇耐药黑色素瘤异种移植小鼠模型中发挥抗肿瘤的活性[1]。

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

Animal Model: NOD scid gamma (NSG) (female, 6−8 weeks old)[1]
Dosage: 10 mg/kg; 15 mg/kg
Administration: i.p.; 3x per week
Result: Reduced mean ex vivo tumor volume and tumor weight.
Decreased Ki67-positive area.
Increased cleaved caspase-3-positive area.
Increased CD45-positive area.
Reduced viable tumor area.
分子量

335.36

Formula

C18H17N5O2
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 polymerization-IN-89 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:

Tubulin polymerization-IN-89Microtubule/TubulinCaspaseApoptosisB16-F10cleaved caspase-3melanoma cellsimmunocompetent mouse modelsmetastatic melanomacleaved PARPA375/TxR cellscolchicine binding sitetubulin heterodimerInhibitorinhibitorinhibit

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