上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。
Tubulin polymerization-IN-4
Tubulin polymerization-IN-4 是一种有效的微管蛋白聚合体 (tubulin polymerization) 抑制剂，IC50 为 4.6 μM。Tubulin polymerization-IN-4 对HeLa细胞可破坏微管蛋白聚合和血管系统，将细胞周期阻滞在G2/M期，诱导细胞凋亡 (apoptosis)，抑制细胞的克隆发生和迁移。
Tubulin polymerization-IN-4 Chemical Structure
| 规格 |
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是否有货 |
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| 100 mg |
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询价 |
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| 250 mg |
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询价 |
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| 500 mg |
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询价 |
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* Please select Quantity before adding items.
| 生物活性 |
Tubulin polymerization-IN-4 is a potent tubulin polymerization inhibitor with IC50 value of 4.6 μM. Tubulin polymerization-IN-4 can disrupt tubulin polymerization and vasculature, arrest the cell cycle at the G2/M phase, induce apoptosis, and suppress clonogenesis and migration in HeLa cells. Tubulin polymerization-IN-4 can be used for researching cervical cancer[1].
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IC50 & Target |
IC50: 4.6 μM (tubulin)[1]
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体外研究
(In Vitro) |
Tubulin polymerization-IN-4 (compound 9j) (0-1 μM; 48 hours) exhibits sub-micromolar inhibitory activities against HeLa, SiHa and MS751[1].
Tubulin polymerization-IN-4 (3, 6 and 12.5 μM; 0-20 min) inhibits tubulin polymerization in a concentration-dependent manner with the inhibition percentages of 39%, 54%, and 77% at 3, 6 and 12.5 μM[1].
Tubulin polymerization-IN-4 (1-100 μM; 2 hours) inhibits the formation of EBI-β-tubulin adduct in a concentration-dependent manner[1].
Tubulin polymerization-IN-4 (0.2 μM; 1 and 2 hours) disrupts the HUVEC-formed vascular tube[1].
Tubulin polymerization-IN-4 (0.1-0.4 μM; 24 hours) increases cell distribution to the G2/M phase in a concentration-dependent manner[1].
Tubulin polymerization-IN-4 (0.1-0.4 μM; 24 hours) induces apoptosis of HeLa cells[1].
Tubulin polymerization-IN-4 (20, 50, 100 nM; 14 days) reduces new colony formation and suppresses HeLa cell growth for 14 days in a dose-dependent manner[1].
Tubulin polymerization-IN-4 (0.1, 0.2 and 0.4 μM; 24 hours) effectively inhibits the migration of HeLa cells in a concentration-dependent manner[1].
Tubulin polymerization-IN-4 (0-200 μM; 24 hours) exhibits good renal safety profile, with IC50 of 188 ± 16 μM in HK-2 cells[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay
| Cell Line: |
HeLa, SiHa and MS751[1] |
| Concentration: |
0-1 μM |
| Incubation Time: |
48 hours |
| Result: |
Exhibited sub-micromolar inhibitory activities against HeLa, SiHa and MS751 with IC50s of 0.09 ± 0.02 μM, 0.15 ± 0.01 μM, 0.11 ± 0.03 μM. |
Cell Cycle Analysis
| Cell Line: |
HeLa cells[1] |
| Concentration: |
0.1, 0.2 and 0.4 μM |
| Incubation Time: |
24 hours |
| Result: |
Increased cell distribution to the G2/M phase in a concentration-dependent way, arresting 24.7%, 47.6% and 71.7% of the cells in this phase at 0.1, 0.2 and 0.4 μM, respectively. |
Apoptosis Analysis
| Cell Line: |
HeLa cells[1] |
| Concentration: |
0.1, 0.2 and 0.4 μM |
| Incubation Time: |
24 hours |
| Result: |
Induced 35.9%, 66.4% and 84.4% of cell population undergoing apoptosis at 0.1 μM, 0.2 μM, 0.4 μM, respectively. |
Cell Cytotoxicity Assay
| Cell Line: |
HK-2 cells[1] |
| Concentration: |
0-200 μM |
| Incubation Time: |
24 hours |
| Result: |
Exhibited good renal safety profile, with IC50 of 188 ± 16 μM in HK-2 cells. |
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体内研究
(In Vivo) |
Tubulin polymerization-IN-4 (100-1000 mg/kg; IP, single) exhibits extremely low toxicity with LD50 over 1000 mg/kg[1].
Tubulin polymerization-IN-4 (30 and 60 mg/kg; IP; daily for 21 days) inhibits the tumor growth, with TGI of 35% and 58% at dosing 30 and 60 mg/kg[1].
Tubulin polymerization-IN-4 (30 mg/kg; IP; single) presents the modest pharmacokinetic properties[1].
Pharmacokinetic Parameters of Tubulin polymerization-IN-4 in ICR mice[1].
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IP (30 mg/kg) |
| T1/2 (h) |
1.56 ± 0.28 |
| Tmax (h) |
0.25 |
| Cmax (μg/L) |
6215 ± 308 |
| AUC0-t (μg/L·h) |
5609 ± 347 |
| AUC0-∞ (μg/L·h) |
5940 ± 347 |
| VZ/F (L/kg) |
11.35 ± 1.29 |
| CLZ/F (L/h/kg) |
5.05 ± 0.91 |
| MRT (h) |
1.77 ± 0.43 |
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
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| 分子量 |
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| Formula |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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| 参考文献 |
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[1]. Huo Z, Liu K, Zhang X, Liang Y, Sun X. Discovery of pyrimidine-bridged CA-4 CBSIs for the treatment of cervical cancer in combination with cisplatin with significantly reduced nephrotoxicity. Eur J Med Chem. 2022;235:114271.
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