AQIM-I is a highly potent small molecule survivin inhibitor by targeting ILF3/NF110, binds to ILF3/NF110 with KD value of 163 nM in SPR assays, has broad-spectrum antitumor activity.
AQIM-I exhibits high antiproliferation potency and excellent selectivity with IC50 values of 0.009 and 21.5 μM against A549 and L929, respectively.
AQIM-I exhibits potent activity against MCF-7 and TE-1, with IC50 values of 0.06 and 0.05 μM, respectively, and considerable potency against H460 (IC50 = 0.14 μM), 5637 (IC50 = 0.18 μM), HepG2 (IC50 = 0.25 μM), H1299 (IC50 = 0.51 μM), and 143B (IC50 = 0.59 μM).
AQIM-I predominantly shows significant antiproliferative activity against cancer cells and low toxicity against normal cells.
AQIM-I produces ROS and causes DNA damage in A549 cells, induces the cell cycle G0/G1 phase arrest, induces apoptosis and autophagy of A549 cells.
AQIM-I attenuates the enhanced survivin promoter activity induced by the overexpression of ILF3/NF110.
AQIM-I (2 mg/kg) markedly inhibits tumor growth in vivo and exhibits greater safety than YM155 and DOX.