2. Cell Cycle/DNA Damage Cytoskeleton Membrane Transporter/Ion Channel Apoptosis
  3. Microtubule/Tubulin P-glycoprotein Apoptosis
  4. Tubulin polymerization/P-gp-IN-1

Tubulin polymerization/P-gp-IN-1 是一种 Tubulin polymerization/P-gp 双重抑制剂。Tubulin polymerization/P-gp-IN-1 可抑制微管蛋白聚合，并诱导 G2/M 期阻滞和细胞凋亡 (apoptosis)。Tubulin polymerization/P-gp-IN-1 通过抑制 P-gp 的外排功能逆转多药耐药性 (MDR)。Tubulin polymerization/P-gp-IN-1 具有双重功能：直接抗肿瘤活性和逆转 P-gp 介导的 Cisplatin (HY-17394) 耐药性。Tubulin polymerization/P-gp-IN-1 可稳定结合微管蛋白的 CBS 结构域 (ΔG = −12.4 kcal/mol) 和 P-gp 的疏水性腔 (ΔG = −10.8 kcal/mol)。Tubulin polymerization/P-gp-IN-1 可用于耐药性宫颈癌的研究。

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Tubulin polymerization/P-gp-IN-1

Tubulin polymerization/P-gp-IN-1 Chemical Structure

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Tubulin polymerization/P-gp-IN-1 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/P-gp-IN-1 is a Tubulin polymerization/P-gp dual inhibitor. Tubulin polymerization/P-gp-IN-1 inhibits tubulin polymerization and induces G2/M arrest and apoptosis. Tubulin polymerization/P-gp-IN-1 reverses MDR by inhibiting P-gp efflux function. Tubulin polymerization/P-gp-IN-1 has dual functions: direct antitumor activity and reversal of P-gp-mediated Cisplatin (HY-17394) resistance. Tubulin polymerization/P-gp-IN-1 stable binds to the tubulin CBS (ΔG = −12.4 kcal/mol) and the P-gp hydrophobic lumen (ΔG = −10.8 kcal/mol). Tubulin polymerization/P-gp-IN-1 can be used for the study of drug-resistant cervical cancer[1].

体外研究
(In Vitro)

Tubulin polymerization/P-gp-IN-1 (Compound 6h) 不仅对 HeLa 细胞 (IC50 = 6.69 μM)、CaSki 细胞 (IC50 = 7.84 μM) 和 SiHa 细胞 (IC50 = 16.68 μM) 等敏感细胞具有高效性，而且对耐药的 HeLa/DDP 细胞系也保持了几乎相同的疗效 (IC50 = 7.21 μM)，并且对人正常宫颈细胞没有明显的细胞毒性 (IC50 = 51.95 μM)[1]。
Tubulin polymerization/P-gp-IN-1 (4-16 μM，24 小时) 可降低聚合的α-和β-微管蛋白水平，同时增加解聚的微管蛋白水平，其作用类似于秋水仙碱 (COL)，但与紫杉醇 (PTX) 相反，并导致微管网络收缩 (尤其是在8 μM和16 μM浓度下)，细胞形态由纺锤形变为圆形，微管仅存在于 HeLa 和 HeLa/DDP 细胞的核周区域[1]。
Tubulin polymerization/P-gp-IN-1 (4-16 μM，24 小时) 不仅可诱导 G2/M 期细胞周期阻滞，还能以浓度依赖的方式有效诱导 HeLa 和 HeLa/DDP 细胞凋亡并显著抑制体外迁移[1]。
Tubulin polymerization/P-gp-IN-1 (0.25 μM、0.5 μM、1 μM，48 小时) 可有效逆转 HeLa/DDP 细胞的 Cisplatin 耐药性[1]。
Tubulin polymerization/P-gp-IN-1 (0.25 μM、0.5 μM、1 μM、12 小时) 不仅浓度依赖性地抑制了 P-gp 介导的外排，而且在 HeLa/DDP 细胞中 1 μM 时保持了 P-gp 蛋白水平不变，并且在 61 ℃ 的高温下显著稳定了 P-gp[1]。

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

Tubulin polymerization/P-gp-IN-1 相关抗体:

Western Blot Analysis[1]

Cell Line: HeLa cells, HeLa/ DDP cells
Concentration: 4 μM, 8 μM, 16 μM
Incubation Time: 24 h
Result: Decreased the levels of polymerized α- and β-tubulin, while the levels of depolymerized tubulin increased, with effects similar to colchicine (COL) but opposite to paclitaxel (PTX).

Cell Cycle Analysis[1]

Cell Line: HeLa cells, HeLa/ DDP cells
Concentration: 4 μM, 8 μM, 16 μM
Incubation Time: 24 h
Result: In the HeLa cells, the proportion of G2/M phase cells increased from 2.98 % (control) to 10.63 % (4 μM), 19.05 % (8 μM) and 30.75 % (16 μM).
In the HeLa/DDP cells, the proportion of G2/M phase cells increased from 7.72 % in the control to 13.41 % (4 μM), 24.05 % (8 μM), and 35.79 % (16 μM).

Apoptosis Analysis[1]

Cell Line: HeLa cells, HeLa/ DDP cells
Concentration: 4 μM, 8 μM, 16 μM
Incubation Time: 24 h
Result: The percentage of apoptotic HeLa cells increased dose-dependently from 4.37 % (control) to 13.15 %, 40.60 %, and 92.80 %, respectively.
HeLa/DDP cells with the apoptotic population increasing from 3.84 % (control) to 10.03 %, 24.76 %, and 67.40 % with 4, 8, and 16 μM, respectively.

Cell Migration Assay [1]

Cell Line: HeLa cells, HeLa/ DDP cells
Concentration: 4 μM, 8 μM, 16 μM
Incubation Time: 24 h
Result: In the HeLa cells, wound closure decreased from 46.59 (control) to 28.11 %, 20.43 %, and 3.35 % with concentrations of 4, 8, and 16 μM.
In the HeLa/DDP cells, wound closure rates decreased from 45.40 % (control) to 24.41 %, 7.47 %, and 1.94 % with concentrations of 4, 8, and 16 μM.
体内研究
(In Vivo)

Tubulin polymerization/P-gp-IN-1 (Compound 6h) (0-400 μM, 96 小时) 即使在斑马鱼胚胎中浓度高达 400 μM 时，仍能保持极佳的安全性 (0% 死亡率；8.3% 畸形率)[1]。

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

658.62

Formula

C36H29F3N2O7
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/P-gp-IN-1 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

Tubulin polymerization/P-gp-IN-1Microtubule/TubulinP-glycoproteinApoptosisP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243Cervical cancerMultidrug resistanceMDRQuinoline-chalconeTubulinInhibitorinhibitorinhibit

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