1449578-65-7

1449578-65-7 structure

Name: AZ82
Chemical Name: AZ82
CAS Number: 1449578-65-7
Molecular Formula: C₂₈H₃₁F₃N₄O₃S
Molecular Weight: 560.63
Catalog: Signaling Pathways Cell Cycle/DNA Damage Kinesin
Create Date: 2019-02-08 18:40:29
Modify Date: 2024-01-20 14:05:39
AZ82 is a selective HSET/KIFC1 inhibitor, with a Ki of 43 nM and an IC50 of 300 nM for KIFC1.

Name	AZ82

Description	AZ82 is a selective HSET/KIFC1 inhibitor, with a Ki of 43 nM and an IC50 of 300 nM for KIFC1.
Related Catalog	Signaling Pathways >> Cell Cycle/DNA Damage >> Kinesin Signaling Pathways >> Cytoskeleton >> Kinesin Research Areas >> Cancer
Target	HSET/KIFC1:300 nM (IC50) HSET/KIFC1:43 nM (Ki)
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[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].
References	[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.