Aurora Kinases-IN-2

Aurora Kinases-IN-2 (compound 12Aj) is a potent Aurora kinases inhibitor with IC50 values of 90 and 152 nM for Aurora A and Aurora B. Aurora Kinases-IN-2 arrests cell cycle at G2/M phase by regulating cyclin B1 and cdc2. Aurora Kinases-IN-2 can be used for cancer research[1].

Signaling Pathways >> Epigenetics >> Aurora Kinase

Research Areas >> Cancer

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

Aurora A:90 nM (IC50)

Aurora B:152 nM (IC50)

Aurora Kinases-IN-2 (compound 12Aj) (72 hours) has antiproliferative activity with IC50 values of 11.5 μM, 1.34 μM, 7.30 μM and 1.64 μM for U87, HeLa, HepG2 and LoVo tumor cell lines, respectively[1]. Aurora Kinases-IN-2 (compound 12Aj) (0-10 μM; 24 hours) inhibits Aurora A and Aurora B in HeLa cells[1]. Aurora Kinases-IN-2 (compound 12Aj) (0-10 μM; 24 hours; HeLa cells) results in G2/M accumulation by regulating the expression of Cyclin B1 and cdc2[1]. Aurora Kinases-IN-2 (compound 12Aj) (0-10 μM; 24 hours) blocks phosphorylation of Aurora kinases in HeLa cells[1]. Western Blot Analysis[1] Cell Line: HeLa cells Concentration: 0, 1, 5 and 10 μM Incubation Time: 24 hours Result: Decreased the expression level of Aurora A and B, as well as reduced phosphorylation of Aurora A on Thr288 (p-Thr288) and Aurora B on Thr232 (p-Thr232) in a dose-dependent manner.

[1]. Bo YX, et, al. Synthesis, biological evaluation and molecular modeling study of 2-amino-3,5-disubstituted-pyrazines as Aurora kinases inhibitors. Bioorg Med Chem. 2020 Mar 1;28(5):115351.