AZ82

AZ82 is a selective HSET/KIFC1 inhibitor, with a Ki of 43 nM and an IC50 of 300 nM for KIFC1.

Signaling Pathways >> Cell Cycle/DNA Damage >> Kinesin

Signaling Pathways >> Cytoskeleton >> Kinesin

Research Areas >> Cancer

HSET/KIFC1:300 nM (IC50)

HSET/KIFC1:43 nM (Ki)

AZ82 is shown to specifically induce multipolar spindles in BT-549 cells, but not in cancer cells with normal centrosome number, such as HeLa[1]. 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 IC50 of 0.90 ± 0.09 μM for mant-ATP binding and 1.26 ± 0.51 μM for mant-ADP releasing[2].

[1]. Godinho SA, et al. Causes and consequences of centrosome abnormalities in cancer. Philos Trans R Soc Lond B Biol Sci. 2014 Sep 5;369(1650).

[2]. Discovery and mechanistic study of a small molecule inhibitor for motor protein KIFC1. Wu J, et al. ACS Chem Biol. 2013 Oct 18;8(10):2201-8.

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