AZ82 is a selective kinesin-like protein KIFC1 (HSET/KIFC1) inhibitor, with a K i of 43 nM and an IC 50 of 300 nM for KIFC1.
In Vitro
AZ82 is shown to specifically induce multipolar spindles in BT-549 cells, but not in cancer cells with normal centrosome number, such as HeLa. AZ82 binds specifically to KIFC1/MT complex but not to KIFC1 or MT alone. Treatment with AZ82 caused centrosome declustering in BT-549 breast cancer cells with amplified centrosomes. AZ82 inhibits both processes with an IC 50 of 0.90 ± 0.09 μM for mant-ATP binding and 1.26 ± 0.51 μM for mant-ADP releasing. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
