Aurora kinase/HDAC-IN-1

Aurora kinase/HDAC-IN-1 is an orally active dual-target inhibitor of Aurora kinase and HDAC. It inhibits Aurora A (IC50 = 116 nM), Aurora B (IC50 = 225 nM), HDAC1 (IC50 = 164 nM), and HDAC2 (IC50 = 346 nM) . This compound enhances histone acetylation (Ac-H3), inhibits phosphorylation of Aurora A and its downstream signaling, and induces apoptosis through G2/M phase arrest. In colorectal cancer cells HCT-116, Aurora kinase/HDAC-IN-1 shows significant antiproliferative activity with an IC50 of 30.2 nM and effectively suppresses tumor growth in HCT-116 colorectal cancer xenograft mouse models.