Tubulin polymerization-IN-11

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].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> Microtubule/Tubulin

Signaling Pathways >> Cytoskeleton >> Microtubule/Tubulin

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]。 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.

[1]. Yang F, et al. Synthesis, and biological evaluation of 3,6-diaryl-[1,2,4]triazolo[4,3-a]pyridine analogues as new potent tubulin polymerization inhibitors. Eur J Med Chem. 2020 Oct 15;204:112625.