2. Cell Cycle/DNA Damage Cytoskeleton Apoptosis NF-κB Metabolic Enzyme/Protease Immunology/Inflammation
  3. Microtubule/Tubulin Apoptosis Reactive Oxygen Species
  4. Tubulin polymerization-IN-6

Tubulin polymerization-IN-6 (化合物 5f) 是一种有效的微管蛋白聚合抑制剂，其IC50 为 1.09 μM。Tubulin polymerization-IN-6 抑制细胞迁移和管的形成，并有助于抗血管生成。Tubulin polymerization-IN-6 可显著抑制 HT29 移植 Balb/c 裸鼠肿瘤生长。

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Tubulin polymerization-IN-6 Chemical Structure

Tubulin polymerization-IN-6 Chemical Structure

CAS No. : 2768613-52-9

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Tubulin polymerization-IN-6 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-6 (compound 5f) is a potent tubulin polymerization inhibitor, with an IC50 of 1.09 μM. Tubulin polymerization-IN-6 inhibits cell migration and tube formation and contributes to the anti-angiogenesis. Tubulin polymerization-IN-6 can greatly inhibit tumor growth on HT29 xenograft Balb/c nude mice[1].

IC50 & Target

IC50: 1.09 μM (Tubulin polymerization)[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
0.24 μM
Compound: 5f
Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
[PMID: 35447432]
HeLa IC50
0.035 μM
Compound: 5f
Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
[PMID: 35447432]
HT-29 IC50
0.023 μM
Compound: 5f
Cytotoxicity against human HT-29 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
Cytotoxicity against human HT-29 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
[PMID: 35447432]
MCF7 IC50
0.14 μM
Compound: 5f
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
[PMID: 35447432]
MDA-MB-231 IC50
0.1 μM
Compound: 5f
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
[PMID: 35447432]
体外研究
(In Vitro)

Tubulin polymerization-IN-6 (compound 5f) (0-20 μM, 24 h) shows a broad spectrum of anti-proliferation activity against cancer cell lines[1].
Tubulin polymerization-IN-6 (0-100 nM, 24 h) inhibits tumor cells colony formation, up-regulates the expression of Ac-α-tubulin and DeY-α-tubulin [1].
Tubulin polymerization-IN-6 (0-5 μM, 1 h) competes with colchicine and directly binds to the colchicine binding site, thus inhibit tubulin polymerization[1].
Tubulin polymerization-IN-6 (0-250 nM, 24 h) possesses a favorable anti-migration activity against cancer cells[1].
Tubulin polymerization-IN-6 (0-50 nM, 24 h) has the ability to inhibit the angiogenesis of HUVEC cells[1].
Tubulin polymerization-IN-6 (0-100 nM, 24 h) induces cell cycle arrest by regulating associated proteins, induces apoptosis by regulating associated proteins and down-regulating mitochondrial membrane potential, and dose-dependently promotes the production of ROS in HT29 cells[1].

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

Tubulin polymerization-IN-6 相关抗体:

Cell Proliferation Assay

Cell Line: HT29, MCF-7, HeLa, MDA-MB-231, A549[1]
Concentration: 0-20 μM
Incubation Time: 24 h
Result: Had a broad spectrum of anti-proliferation activity against cancer cell lines (MCF-7, MDA-MB-231, A549, Hela, and HT29), with IC50 values of 0.14 ± 0.03, 0.10 ± 0.00, 0.24 ± 0.03, 0.035 ± 0.002, and 0.023 ± 0.001 μM, respectively; and showed moderate anti-proliferative activity against drug resistant cancer cells (MCF-7/TxR and A549/TxR), with IC50 values of 0.18 ± 0.02 and 0.31 ± 0.08 μM, and DRI (drug-resistant index) of 1.3 and 1.2, respectively.

Western Blot Analysis

Cell Line: HT29 cells[1]
Concentration: 0, 25, 50, and 100 nM
Incubation Time: 24 h
Result: Up-regulated the expression of Ac-α-tubulin (acetyl-α-tubulin) and DeY-α-tubulin (detyrosinated-α-tubulin); regulated the expressions of the proteins involved in cell cycle such as cdc25c, cdk7, cyclin B1, and cdc2; down-regulated the level of Bim and up-regulated the levels of Bcl-2, p-Bcl-2, and Bax, decreased the expression of p-Histone H3(Ser10) and increased the expression of cleaved-Caspase-9, cleaved-Caspase-3, PARP, and cleaved-PARP.

Immunofluorescence

Cell Line: HT29 cells[1]
Concentration: 0, 25, 50, and 100 nM
Incubation Time: 6 h
Result: Dose-dependently depolymerized the tubulin polymers into oligomers, and caused the microtubule network to collapse in HT29 cells.

Cell Cycle Analysis

Cell Line: HT29 cells[1]
Concentration: 0, 12.5, 25, 50, and 100 nM
Incubation Time: 24 h
Result: Induced a dose dependent G2/M phase arrest, increased the proportion of G2/M phase cells from 20.9% to 87.5% at 100 nM.

Apoptosis Analysis

Cell Line: HT29 cells[1]
Concentration: 0, 25, 50, and 100 nM
Incubation Time: 24 h
Result: Induced apoptosis, increased the percentages of total apoptosis cells, down-regulated mitochondrial membrane potential.
体内研究
(In Vivo)

Tubulin polymerization-IN-6 (compound 5f) (HT29 xenograft Balb/c nude mice, 0-10 mg/kg, IP, once every two days, for three weeks) dose-dependently inhibits the tumor growth[1].
Tubulin polymerization-IN-6 (SD rats, 10 mg/kg, IV, once) shows the better pharmacokinetic properties[1]. Pharmacokinetic Parameters of Tubulin polymerization-IN-6 in SD rats[1].

Parameters 5f
t1/2 (h) 1.73
AUC (μg/L·h) 5.67
MRT (h) 1.92
CL (L/h/kg) 1.76
Tmax (h) 0.14
Cmax (ng/mL) 6.88

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

Animal Model: Immunodeficient Balb/c nude mice (HT29 xenograft, 5-week-old, 36 mice, six groups)[1]
Dosage: 0, 5, 7.5, 10 mg/kg
Administration: IP, once every two days, for three weeks
Result: Dose-dependently inhibited the tumor growth, inhibits the tumor weight growth by 75.5% at 10 mg/kg.
Animal Model: SD rats (5-week-old)[1]
Dosage: 10 mg/kg
Administration: IV, once (Pharmacokinetic Analysis)
Result: Showed the better pharmacokinetic properties, exhibited an eight-fold half-life and a two-fold AUC improvement.
分子量

375.37

Formula

C19H21NO7
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-6 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

Tubulin polymerization-IN-62768613-52-9Microtubule/TubulinApoptosisReactive Oxygen SpeciesHT29 cellsLow toxicityAntitumor activityInhibitorinhibitorinhibit

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