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-9
Tubulin polymerization-IN-9 是一种有效的微管蛋白 (tubulin) 抑制剂，IC50 为 1.82 μM。Tubulin polymerization-IN-9 能引起细胞周期阻滞在 G2/M 期，诱导 K562 细胞凋亡 (apoptosis) 和线粒体去极化。Tubulin polymerization-IN-9 具有强效的抗血管和抗肿瘤活性。
Tubulin polymerization-IN-9 Chemical Structure
CAS No. : 2485020-93-5
| 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-9 is a potent tubulin inhibitor with IC50 of 1.82 μM. Tubulin polymerization-IN-9 causes cell cycle arrest at G2/M phase, and induces cell apoptosis and depolarized mitochondria of K562 cells. Tubulin polymerization-IN-9 has potent anti-vascular and antitumor activities[1].
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IC50 & Target |
IC50: 1.82 μM (tubulin)[1]
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体外研究
(In Vitro) |
Tubulin polymerization-IN-9 (compound 11k) (0.1, 1, 10 μM; 72 hours) has potent activity against these three cancer cell lines with IC50 values ranging from 0.287 to 0.621 μM[1].
Tubulin polymerization-IN-9 (0.15, 0.3 and 0.6 μM; 24 hours) induces a dose-dependent collapse of the microtubule networks[1].
Tubulin polymerization-IN-9 (0.15, 0.3 and 0.6 μM; 48 hours) observes a gradual accumulation of cells at G2/M phase in K562 cells[1].
Tubulin polymerization-IN-9 (0.15, 0.3 and 0.6 μM; 72 hours) effectively induces cell apoptosis in K562 cells in a concentration-dependent manner[1].
Tubulin polymerization-IN-9 (0.15, 0.3 and 0.6 μM; 24 hours) causes mitochondrial depolarization of K562 cells in the process of apoptosis[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay
| Cell Line: |
K562 HepG2 and HCT-8 cells[1] |
| Concentration: |
0.1, 1, 10 μM |
| Incubation Time: |
72 hours |
| Result: |
Showed potent activity against these three cancer cell lines with IC50 values ranging from 0.287 to 0.621 μM. |
Immunofluorescence
| Cell Line: |
K562 cells[1] |
| Concentration: |
0.15, 0.3 and 0.6 μM |
| Incubation Time: |
24 hours |
| Result: |
Induced a dose-dependent collapse of the microtubule networks. |
Cell Cycle Analysis
| Cell Line: |
K562 cells[1] |
| Concentration: |
0.15, 0.3 and 0.6 μM |
| Incubation Time: |
48 hours |
| Result: |
Observed a gradual accumulation of cells at G2/M phase in K562 cells. |
Apoptosis Analysis
| Cell Line: |
K562 cells[1] |
| Concentration: |
0.15, 0.3 and 0.6 μM |
| Incubation Time: |
72 hours |
| Result: |
Effectively induced cell apoptosis in K562 cells in a concentration-dependent manner. |
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体内研究
(In Vivo) |
Tubulin polymerization-IN-9 (15 and 30 mg/kg; IV; once a day, for 21 days) effectively suppresses the tumor volume and reduces tumor weight by 71.1% at a dose of 30 mg/kg[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: |
Male ICR mice (5 weeks; injected with H22 cells; n=6)[1] |
| Dosage: |
15 and 30 mg/kg |
| Administration: |
IV; once a day, for 21 days |
| Result: |
Effectively suppressed the tumor volume and reduced tumor weight by 71.1% at a dose of 30 mg/kg. |
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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]. Zhu H, Sun H, Liu Y, et al. Design, synthesis and biological evaluation of vinyl selenone derivatives as novel microtubule polymerization inhibitors. Eur J Med Chem. 2020;207:112716.
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