For research use only. Not for therapeutic Use.
AZ82 is a selective kinesin-like protein KIFC1 (HSET/KIFC1) inhibitor, with a Ki of 43 nM and an IC50 of 300 nM for KIFC1.
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].
| Catalog Number | R067053 |
| CAS Number | 1449578-65-7 |
| Synonyms | 5-methyl-N-[(2R)-1-oxo-1-[[(3R)-pyrrolidin-3-yl]amino]-3-[6-[3-(trifluoromethoxy)phenyl]pyridin-3-yl]propan-2-yl]-4-propylthiophene-2-carboxamide |
| Molecular Formula | C28H31F3N4O3S |
| Purity | ≥95% |
| InChI | InChI=1S/C28H31F3N4O3S/c1-3-5-19-14-25(39-17(19)2)27(37)35-24(26(36)34-21-10-11-32-16-21)12-18-8-9-23(33-15-18)20-6-4-7-22(13-20)38-28(29,30)31/h4,6-9,13-15,21,24,32H,3,5,10-12,16H2,1-2H3,(H,34,36)(H,35,37)/t21-,24-/m1/s1 |
| InChIKey | PMTLKNOARSHUJB-ZJSXRUAMSA-N |
| SMILES | CCCC1=C(SC(=C1)C(=O)NC(CC2=CN=C(C=C2)C3=CC(=CC=C3)OC(F)(F)F)C(=O)NC4CCNC4)C |
| Reference | [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. |
