2. Cell Cycle/DNA Damage Cytoskeleton Apoptosis
  3. Microtubule/Tubulin Apoptosis
  4. 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。

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Tubulin polymerization-IN-4 Chemical Structure

Tubulin polymerization-IN-4 Chemical Structure

CAS No. : 2835559-00-5

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Tubulin polymerization-IN-4 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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].

IC50 & Target

IC50: 4.6 μM (tubulin)[1]
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].

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

Tubulin polymerization-IN-4 相关抗体:

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.
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].

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

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

400.86

Formula

C21H21ClN2O4
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-4 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

Tubulin polymerization-IN-42835559-00-5Microtubule/TubulinApoptosisCervical cancerAnti-tumorHeLa cellsBalb/c nude miceC57 nude miceInhibitorinhibitorinhibit

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