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AZ82

Chemical Structure : AZ82

CAS No.: 1449578-65-7

AZ82 (KIFC1 inhibitor AZ82)

Catalog No.: PC-62374Not For Human Use, Lab Use Only.

AZ82 (KIFC1 inhibitor AZ82) is the first reported small molecule inhibitor of motor protein KIFC1 that inhibits the MT-stimulated KIFC1 enzymatic activity in an ATP-competitive and MT-noncompetitive manner with Ki of 43 nM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

AZ82 (KIFC1 inhibitor AZ82) is the first reported small molecule inhibitor of motor protein KIFC1 that inhibits the MT-stimulated KIFC1 enzymatic activity in an ATP-competitive and MT-noncompetitive manner with Ki of 43 nM; effectively engages with the minus end-directed KIFC1 motor inside cells to reverse the monopolar spindle phenotype induced by the inhibition of the plus end-directed kinesin Eg5; causes centrosome declustering in BT-549 breast cancer cells with amplified centrosomes.

Physicochemical Properties

M.Wt 560.6
Formula C28H31F3N4O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

5-methyl-N-((R)-1-oxo-1-(((R)-pyrrolidin-3-yl)amino)-3-(6-(3-(trifluoromethoxy)phenyl)pyridin-3-yl)propan-2-yl)-4-propylthiophene-2-carboxamide

References

1. Wu J, et al. ACS Chem Biol. 2013 Oct 18;8(10):2201-8.

2. Yang B, et al. J Med Chem. 2014 Dec 11;57(23):9958-70.

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