Bioactivity | 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]. |
Invitro | 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: |
Name | Tubulin polymerization-IN-11 |
CAS | 2470063-59-1 |
Formula | C22H22N4O4 |
Molar Mass | 406.43 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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. |