AZ82

Modify Date: 2024-01-20 14:05:39

AZ82 Structure
AZ82 structure
Common Name AZ82
CAS Number 1449578-65-7 Molecular Weight 560.63
Density N/A Boiling Point N/A
Molecular Formula C28H31F3N4O3S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of AZ82


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

 Names

Name AZ82

 AZ82 Biological Activity

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

 Chemical & Physical Properties

Molecular Formula C28H31F3N4O3S
Molecular Weight 560.63
Storage condition 2-8℃