1. Cell Cycle/DNA Damage Cytoskeleton Apoptosis
  2. Microtubule/Tubulin Apoptosis
  3. Tubulin polymerization-IN-11

Tubulin polymerization-IN-11 是一种有效的微管蛋白聚合 (tubulin polymerization) 抑制剂,IC50 值为 3.4 µM。Tubulin polymerization-IN-11 显示出抗增殖活性。Tubulin polymerization-IN-11 诱导细胞凋亡 (Apoptosis) 和细胞周期停滞在 G2/M 期。Tubulin polymerization-IN-11 降低cyclin B1, p-cdc2 和 Bcl-2 蛋白表达并增加 cleaved PARP 的表达。

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Tubulin polymerization-IN-11 Chemical Structure

Tubulin polymerization-IN-11 Chemical Structure

CAS No. : 2470063-59-1

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Tubulin polymerization-IN-11 is a potent tubulin polymerization inhibitor with an IC50 value of 3.4 µM. Tubulin polymerization-IN-11 shows antiproliferative activity. Tubulin polymerization-IN-11 induces Apoptosis and cell cycle arrest at G2/M phase. Tubulin polymerization-IN-11 decreases the expression of cyclin B1, p-cdc2, and Bcl-2 protein levels and increases the expression of cleaved PARP[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
10.4 μM
Compound: 7i
Antiproliferative activity against human A549 cells measured after 48 hrs by MTT assay
Antiproliferative activity against human A549 cells measured after 48 hrs by MTT assay
[PMID: 32717486]
HEK293 IC50
> 100 μM
Compound: 7i
Cytotoxicity against HEK293 cells measured after 48 hrs by MTT assay
Cytotoxicity against HEK293 cells measured after 48 hrs by MTT assay
[PMID: 32717486]
HeLa IC50
0.012 μM
Compound: 7i
Antiproliferative activity against human HeLa cells measured after 48 hrs by MTT assay
Antiproliferative activity against human HeLa cells measured after 48 hrs by MTT assay
[PMID: 32717486]
HeLa IC50
0.012 μM
Compound: 6
Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth by MTT assay
Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth by MTT assay
[PMID: 36089111]
MCF7 IC50
40.4 μM
Compound: 7i
Antiproliferative activity against human MCF7 cells measured after 48 hrs by MTT assay
Antiproliferative activity against human MCF7 cells measured after 48 hrs by MTT assay
[PMID: 32717486]
T47D IC50
27.91 μM
Compound: 7i
Antiproliferative activity against human T47D cells measured after 48 hrs by MTT assay
Antiproliferative activity against human T47D cells measured after 48 hrs by MTT assay
[PMID: 32717486]
体外研究
(In Vitro)

Tubulin polymerization-IN-11 (compound 7i) (0-100 µM; 48 h) 显示抗增殖活性,对HeLa, HEK-293, A549, MCF-7, T47D 细胞的 IC50 值分别为 0.012、>100 µM、10.40、40.40、27.91 µM[1].
Tubulin polymerization-IN-11 (12, 24, 48 nM; 24 h) 以剂量依赖的方式诱导细胞凋亡和细胞周期停滞在 G2/M 期[1]
Tubulin polymerization-IN-11 (12, 24, 48 nM; 24 h) 以剂量依赖性方式降低细胞周期蛋白 B1、p-cdc2、Bcl-2 蛋白水平并增加 cleaved PARP 蛋白的表达[ 1]

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

Cell Proliferation Assay[1]

Cell Line: HeLa, HEK-293, A549, MCF-7, T47D cells
Concentration: 0-100 µM
Incubation Time: 48 h
Result: Showed antiproliferative activity with IC50s of 0.012, >100, 10.40, 40.40, 27.91 µM for HeLa, HEK-293, A549, MCF-7, T47D cells, respectively.

Cell Cycle Analysis[1]

Cell Line: HeLa cells
Concentration: 12, 24, 48 nM
Incubation Time: 24 h
Result: Induced cell cycle arrest at G2/M phase with the percentage of cells was 13.90%, 26.00%, and 92.65% at 12, 24, 48 nM, respectively.

Western Blot Analysis[1]

Cell Line: HeLa cells
Concentration: 12, 24, 48 nM
Incubation Time: 24 h
Result: Concentration-dependently decreased cyclin B1 and p-cdc2 protein levels.

Apoptosis Analysis[1]

Cell Line: HeLa cells
Concentration: 12, 24, 48 nM
Incubation Time: 24 h
Result: Induced apoptosis with the total numbers of early and late apoptotic cells were 8.44%, 26.87% and 53.3% at 12, 24, and 48 nM, respectively.
分子量

406.43

Formula

C22H22N4O4

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
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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