Aurora A inhibitor 2

Aurora A inhibitor 2 (Compound 16h) is a potent Aurora A kinase inhibitor with an IC50 of 21.94 nM. Aurora A inhibitor 2 induces caspase-dependent apoptosis in MDA-MB-231 cells[1].

Signaling Pathways >> Epigenetics >> Aurora Kinase

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> Aurora Kinase

Aurora A:21.94 nM (IC50)

Aurora B:273.18 nM (IC50)

Aurora A inhibitor 2 (Compound 16h) (0-20 µM, 48 h) shows potent antiproliferative activity against various human cancer cells, and inhibits colony formation[1]. Aurora A inhibitor 2 (0-4 µM, 24 h) inhibits the expression of phosphorylation of Aurora A and Histone H3 in a dose-dependent manner, and induces G2/M cell cycle arrest [1]. Aurora A inhibitor 2 (0-4 µM, 48 h) induces obvious apoptosis in MDA-MB-231 cells in a concentration-dependent manner[1]. Cell Cytotoxicity Assay[1] Cell Line: Breast cancer MDA-MB231, prostate cancer PC3, and neuroblastoma SH-SY5Y cells Concentration: 0-20 µM Incubation Time: 48 h Result: Displayed potent antiproliferative activity with IC50 values of 0.38 ± 0.08, 1.09 ± 0.24, and 0.77 ± 0.12 µM against MDA-MB-231, PC3, and SH-SY5Y cells. Western Blot Analysis[1] Cell Line: MDAMB-231 Concentration: 1, 2, and 4 µM Incubation Time: 24 h Result: A dose-dependent and significant reduction in the phosphorylation of Aurora A and Histone H3 was observed. Significantly increased the levels of cleaved caspase 3/9 and cleaved-PARP. Cell Cycle Analysis[1] Cell Line: MDAMB-231 Concentration: 1, 2, and 4 µM Incubation Time: 24 h Result: Dose-dependently increased the and population of cells in the G2/M phase. Apoptosis Analysis[1] Cell Line: MDAMB-231 Concentration: 1, 2, and 4 µM Incubation Time: 48 h Result: Induced obvious apoptosis in a concentration-dependent manner.

[1]. Chengcheng Fan, et al. Design, synthesis, biological evaluation of 6-(2-amino-1H-benzo[d]imidazole-6-yl)quinazolin-4(3H)-one derivatives as novel anticancer agents with Aurora kinase inhibition. Eur J Med Chem. 2020 Mar 15;190:112108.