2. Cell Cycle/DNA Damage Cytoskeleton Metabolic Enzyme/Protease Apoptosis NF-κB Immunology/Inflammation
  3. Microtubule/Tubulin MMP Bcl-2 Family Reactive Oxygen Species (ROS) Caspase
  4. Tubulin polymerization-IN-82

Tubulin polymerization-IN-82 是一种微管蛋白 (tubulin) 抑制剂。能够抑制细胞迁移和侵袭，并通过线粒体和内质网应激介导的途径引发细胞凋亡 (apoptosis)。Tubulin polymerization-IN-82 对耐药癌细胞具有抗肿瘤活性，并抑制肿瘤生长，可用于肝癌研究[1]。

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Tubulin polymerization-IN-82 Chemical Structure

Tubulin polymerization-IN-82 Chemical Structure

CAS No. : 3067075-77-5

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Tubulin polymerization-IN-82 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Tubulin polymerization-IN-82 is a tubulin inhibitor. Inhibits cell migration and invasion, and triggers cell apoptosis through the mitochondria and ER stress mediated pathway. Tubulin polymerization-IN-82 exhibits antitumor activity against drug resistance cancer cells, and inhibits tumor growth, can be used for liver cancer research[1].

体外研究
(In Vitro)

Tubulin polymerization-IN-82 (Compound 9n) (0.039-2.5 μM， 72 h) 对不同细胞表现出抗增殖活性，IC50 分别为 0.09 μM (HepG-2) 、0.25 μM (NCI-H460) 、0.20 μM (HCT-116) 、0.18 μM (SK-OV-3)[1]。

Tubulin polymerization-IN-82 (0.039-2.5 μM, 72 h) 对耐药细胞具有抗增殖作用，IC50 分别为 0.29 μM (A549/CDDP) 、0.45 μM (A549/紫杉醇) 、0.51 μM (MCF-7/DOX)[1]。

ubulin polymerization-IN-82 (1.25-20 μM, 5-65 min) 可抑制纯化微管蛋白的微管蛋白聚合，IC50 为 3.56 μM[1]。

Tubulin polymerization-IN-82 (1.25 μM, 2.5 μM, 24 h) 通过线粒体介导的途径和内质网应激破坏 HepG-2 细胞中的微管网络诱导HepG-2 细胞凋亡[1]。

Tubulin polymerization-IN-82 (1.25 μM, 2.5 μM, 24 h) 可使 HepG-2 细胞周期停滞于 G2/M 期，且呈浓度依赖性[1]。

Tubulin polymerization-IN-82 (1.25 μM, 2.5 μM, 24 h) 可降低 HepG-2 细胞的基质金属蛋白酶 (MMP)，诱导活性氧 (ROS) 生成[1]。

Tubulin polymerization-IN-82 (1.25 μM, 2.5 μM, 24 h) 可提高 HepG-2 细胞内 Ca2+ 水平，并增加 p-PERK、p-eIF2α 和 CHOP 的表达水平[1]。

[1]。

Tubulin polymerization-IN-82 在羧酸酯酶作用 4 小时后被酯酶水解[1]。

Tubulin polymerization-IN-82 在 PBS (pH = 7.4) 和含有 1% DMF 的 DMEM 培养基中，24、48 或 72 小时后仍保持稳定[1]。

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

Tubulin polymerization-IN-82 相关抗体:

Apoptosis Analysis[1]

Cell Line: HepG-2 cells
Concentration: 1.25 and 2.5 μM
Incubation Time: 24 h
Result: Accounted for 13.76% and 31.2% of apoptotic cells (including early and late apoptotic cells). At the same concentration, apoptosis was induced more effectively by 9n (31.2%) than by CA-4 (20.18%).
Reduced the expression levels of cyclin B1, Cdc25c, and Cdc2 in HepG-2 cells.
Downregulated the expression of the anti-apoptotic protein Bcl-2 and upregulated the expression of the pro-apoptotic protein Bax in HepG-2 cells, activated the expression level of caspase-3 protein, triggered apoptosis in HepG-2 cells.

Cell Cycle Analysis[1]

Cell Line: HepG-2 cells
Concentration: 1.25 and 2.5 μM
Incubation Time: 24 h
Result: Caused cell cycle arrest at the G2/M phase.
Reduced expression levels of cyclin B1, Cdc25c, and Cdc2.
体内研究
(In Vivo)

Tubulin polymerization-IN-82 (Compound 9n) (15 或 30 mg/kg，腹腔注射，21 天) 抑制 HepG-2 异种移植模型中的肿瘤生长[1]。

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

Animal Model: HepG-2 xenograft models in (Balb/c-nu) mice (6-week-old)[1].
Dosage: 15 or 30 mg/kg
Administration: i.v. ,for 21 days
Result: Inhibited tumor growth with the tumor growth inhibition (TGI) rates of 58.3% and 70.7%, respectively.
Not changed the body weight of the mice.
Not changed histopathology in the liver, heart, lung, spleen and kidney.
分子量

520.57

Formula

C30H32O8
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

Tubulin polymerization-IN-82 相关分类

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Keywords:

Tubulin polymerization-IN-823067075-77-5Microtubule/TubulinMMPBcl-2 FamilyReactive Oxygen Species (ROS)CaspaseMatrix metalloproteinasesTubulin inhibitorpro-apoptosisanti-tumorA549/CDDPHepG-2HepG-2 xenograft modeldrug resistanceHepatocellular carcinomaHCCInhibitorinhibitorinhibit

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