2. Cell Cycle/DNA Damage Cytoskeleton Apoptosis
  3. Microtubule/Tubulin Apoptosis Bcl-2 Family
  4. Tubulin polymerization-IN-88

Tubulin polymerization-IN-88 是一种微管蛋白 (tubulin) 抑制剂，可阻断微管蛋白聚合，引发微管去稳定化和有丝分裂纺锤体破坏。Tubulin polymerization-IN-88 可诱导癌细胞发生 G2/M 期阻滞，并诱导细胞凋亡 (apoptosis)，抑制癌细胞迁移和癌症干细胞的自我更新。Tubulin polymerization-IN-88 对癌细胞具有体外抗增殖活性，且相较于正常细胞具有选择性。Tubulin polymerization-IN-88 具有体内抗癌活性，且无明显毒性。Tubulin polymerization-IN-88 可用于胶质母细胞瘤、肺癌、子宫内膜癌、卵巢癌、白血病的研究。

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Tubulin polymerization-IN-88

Tubulin polymerization-IN-88 Chemical Structure

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Tubulin polymerization-IN-88 相关抗体

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查看 Bcl-2 Family 亚型特异性产品:

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Tubulin polymerization-IN-88 is a tubulin inhibitor that blocks tubulin polymerization, leading to microtubule destabilization and disruption of the mitotic spindle. Tubulin polymerization-IN-88 induces G2/M phase arrest and apoptosis in cancer cells, and inhibits cancer cell migration and self-renewal of cancer stem cells. It exhibits in vitro anti-proliferative activity against cancer cells with selectivity over normal cells. Tubulin polymerization-IN-88 also demonstrates in vivo anti-cancer activity without significant toxicity. Tubulin polymerization-IN-88 is applicable for research on glioblastoma, lung cancer, endometrial cancer, ovarian cancer, and leukemia[1].

IC50 & Target[1]

Bcl-xL

 

体外研究
(In Vitro)

Tubulin polymerization-IN-88 (compound 9b) (作用时间 72 h) 可强效抑制胶质母细胞瘤 (U87 MG、A172、U118 MG)、肺癌 (A549)、卵巢癌 (SKOV3)、白血病 (K562、HL60) 等多种癌细胞系的增殖，其 IC50 值范围为 0.27 至 12.45 μM，同时对正常 293T 细胞无毒性[1]。
Tubulin polymerization-IN-88 (1-30 μM；作用 24 h) 可在浓度 ≥3 μM 时诱导 U118 MG 细胞发生剂量依赖性凋亡，并下调 Bcl-XL 的表达[1]。
Tubulin polymerization-IN-88 (0.1-1 μM；24-72 h) 通过划痕伤口愈合实验和 Transwell 实验，以浓度和时间依赖的方式强效抑制 U118 MG 细胞的迁移[1]。
Tubulin polymerization-IN-88 (1-30 μM；处理 3 天) 可通过降低神经球形成能力并下调 CD133 和 SOX2 的表达，有效抑制 U118 MG 癌症干细胞的自我更新[1]。
Tubulin polymerization-IN-88 (1-30 μM；作用 24 h) 可通过下调 Cyclin B1 和 CDK1 诱导 U118 MG 细胞发生 G2/M 期阻滞[1]。
Tubulin polymerization-IN-88 (1-30 μM；作用 24 h) 可破坏 U118 MG 细胞中的微管蛋白聚合及纺锤体微管组装，进而降低 α/β-微管蛋白的表达[1]。

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

Tubulin polymerization-IN-88 相关抗体:

Cell Viability Assay[1]

Cell Line: U87 MG, A172, U118 MG, A549, ISK, SKOV3, U251, K562, HL60, 293T
Concentration: varied for IC₅₀ determination
Incubation Time: 72 h
Result: Inhibited proliferation of U87 MG cells with an IC50 of 0.27 μM; inhibited proliferation of A172 cells with an IC50 of 1.22 μM; inhibited proliferation of U118 MG cells with an IC50 of 0.88 μM; inhibited proliferation of A549 cells with an IC50 of 0.33 μM; inhibited proliferation of ISK cells with an IC50 of 12.45 μM; inhibited proliferation of SKOV3 cells with an IC50 of 0.47 μM; inhibited proliferation of U251 cells with an IC50 of 1.29 μM; inhibited proliferation of K562 cells with an IC50 of 0.73 μM; inhibited proliferation of HL60 cells with an IC50 of 2.02 μM; showed negligible toxicity to 293T cells with an IC50 >100 μM.

Apoptosis Analysis[1]

Cell Line: U118 MG
Concentration: 1, 3, 10, 30 μM
Incubation Time: 24 h
Result: Induced dose-dependent increase in total apoptotic cells, with statistical significance at and above 3 μM; downregulated anti-apoptotic protein Bcl-XL in a concentration-dependent manner.

Cell Migration Assay [1]

Cell Line: U118 MG
Concentration: 0.1, 0.3, 1 μM
Incubation Time: 24, 48, 72 h (scratch assay); 24 h (transwell assay)
Result: Inhibited scratch wound closure in a concentration- and time-dependent manner (significant inhibition at 72 h); dose-dependently reduced transwell migration.

Cell Cycle Analysis[1]

Cell Line: U118 MG
Concentration: 1, 3, 10, 30 μM
Incubation Time: 24 h
Result: Induced G2/M phase arrest at low concentrations (1-10 μM); dose-dependently reduced expression of cell cycle regulators Cyclin B1 and CDK1.

Western Blot Analysis[1]

Cell Line: U118 MG
Concentration: 1, 3, 10, 30 μM
Incubation Time: 24 h
Result: Significantly reduced α/β-tubulin protein
expression in U118 MG cells.
药代动力学
(Parmacokinetics)
Species Dose Route Cmax Tmax AUC0-inf T1/2 MRT0-inf F
Rat[1] 5 mg/kg i.v. 3241 ng/mL / 651 ng·h/mL 1.03 h 0.264 h /
Rat[1] 10 mg/kg i.p. 271 ng/mL 0.25 h 407 ng·h/mL 1.20 h 1.46 h 40.8 %
体内研究
(In Vivo)

Tubulin polymerization-IN-88 (compound 9b) (2.5-20 mg/kg; i.p.; daily; 28 days) 在体内表现出强效的剂量依赖性抗胶质母细胞瘤活性，肿瘤重量生长抑制率 (TGI) 为 49.7-49.8%，且具有可接受的安全性特征[1]。

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

Animal Model: BALB/c nude (male, 6-7 weeks old, 16-19 g, U118 MG xenograft model)[1]
Dosage: 2.5, 8, 20 mg/kg
Administration: i.p.; daily; 28 days
Result: Suppressed tumor growth dose-dependently; induced 49.7% tumor weight growth inhibition (TGI) at 8 mg/kg, and 49.8% TGI at 20 mg/kg (both statistically significant vs control); caused no significant body weight loss or overt toxicity.
分子量

521.71

Formula

C30H39N3O3S
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-88 相关分类

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Keywords:

Tubulin polymerization-IN-88Microtubule/TubulinApoptosisBcl-2 Familyendometrial cancercancer stem cellsG2/M-phase arrestlung cancermitotic spindleglioblastomaovarian cancermicrotubuletubulinleukemiaInhibitorinhibitorinhibit

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