Tubulin polymerization-IN-26

Tubulin polymerization-IN-26 (compound 12h) can inhibit the polymerization of microtubulin by binding to the colchicine binding site of microtubulin with an IC50 value of 4.64 μM. Tubulin polymerization-IN-26 can induce apoptosis and inhibit cell metastasis or migration, and can be used as a potential compound for lung cancer research[1].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

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

Signaling Pathways >> Cytoskeleton >> Microtubule/Tubulin

Tubulin polymerization-IN-26 (compound 12h) (0.27-30 μM, 48 hours) shows potent cytotoxic activity against lung cancer cells[1]. Tubulin polymerization-IN-26 (compound 12h) (0.1 μM,0.25 μM,0.5 μM, 24 hours) induces cell apoptosis in a dose-dependent manner by promoting ROS production in cells [1]. Tubulin polymerization-IN-26 (compound 12h) (0.1 μM,0.25 μM,0.5 μM, 24 hours) arrests the cell cycle in G2/M phase[1]. Tubulin polymerization-IN-26 (compound 12h) (0.1 μM,0.25 μM,0.5 μM, 24 hours) inhibits microtubule protein polymerization[1]. Cell Cytotoxicity Assay[1] Cell Line: Human non-small cell lung cancer A549, Human triple negative breast cancer MDA-MB-231, Mouse melanoma B16-F10, Human breast cancer BT-474, Mouse triple negative breast cancer 4 T1, Rat kidney epithelial cell line NRK-52E Concentration: 0.27-30 μM Incubation Time: 48 hours Result: Showed cytotoxic activity against A549, MDA-MB-231, B16-F10, BT-474, 4 T1, NRK-52E with IC50 value of 0.29 μM,1.48 μM,1.25 μM,0.42 μM,0.49 μM,1.58 μM respectively. Apoptosis Analysis[1] Cell Line: Human non-small cell lung cancer A549 Concentration: 0.1 μM,0.25 μM,0.5 μM Incubation Time: 24 hours Result: Changed cell nucleus from normal form to micronucleus with the concentration increasing. Cell Cycle Analysis[1] Cell Line: Human non-small cell lung cancer A549 Concentration: 0.1 μM,0.25 μM,0.5 μM Incubation Time: 24 hours Result: Resulted in more G2/M phase cells production which percentage were 17.6%, 29% and 50.3%, corresponding to concentrations of 0.1 μM, 0.25 μM, and 0.5 μM, respectively. Resulted in even fewer G0/G1 phase cells production which percentage were 41. 1%, 21.2%, and 4.9%, corresponding to concentrations of 0.1 μM, 0.25 μM, and 0.5 μM, respectively.

[1]. Kavitha Donthiboina，et al. Synthesis and biological evaluation of substituted N-(2-(1H-benzo[d]imidazol-2-yl)phenyl)cinnamides as tubulin polymerization inhibitors. Bioorg Chem. 2020 Oct;103:104191.