AZ82 is a small molecule inhibitor of KIFC1/HSET, a kinesin-14 family protein that is important for assembling bipolar spindles in cancer cells containing supernumerary centrosomes.
CAS:1449578-65-7
分子式:C28H31F3N4O3S
分子量:560.6
纯度:98%
存储:Store at -20°C
Background:
AZ82 is a small molecule inhibitor of KIFC1/HSET, a kinesin-14 family protein that is important for assembling bipolar spindles in cancer cells containing supernumerary centrosomes. AZ82 binds to the KIFC1/microtubule complex and inhibits its microtubule-stimulated activity (IC50 = 300 nM) in an ATP-competitive (Ki = 43 nM) and microtubule-noncompetitive manner but does not inhibit basal KIFC1 activity at a concentration of 100 uM. It is selective for KIFC1 over a panel of nine kinesin motor proteins at a concentration of 5 uM. AZ82 induces multipolar spindle formation in cancer cell lines with high (BT549), but not low (HeLa and MCF-7), numbers of extra chromosomes.