An inhibitor of KIFC1; binds to the KIFC1/microtubule complex and inhibits its microtubule-stimulated activity (IC50 = 300 nM) in an ATP-competitive (Ki = 43 nM) and microtubule-noncompetitive manner; does not inhibit basal KIFC1 activity at a concentration of 100 µM; selective for KIFC1 over a panel of nine kinesin motor proteins at a concentration of 5 µM; AZ82 preferentially induces multipolar spindle formation in cancer cell lines with high numbers of extra chromosomes

AZ82 – 5 mg

Brand:
Cayman
CAS:
1449578-65-7
Storage:
-20
UN-No:
Non-Hazardous - /

AZ82 is a small molecule inhibitor of KIFC1/HSET, a kinesin-14 family protein that is important for assembling bipolar spindles in cancer cells containing supernumerary centrosomes.{38506} AZ82 binds to the KIFC1/microtubule complex and inhibits its microtubule-stimulated activity (IC50 = 300 nM) in an ATP-competitive (Ki = 43 nM) and microtubule-noncompetitive manner but does not inhibit basal KIFC1 activity at a concentration of 100 µM.{38507} It is selective for KIFC1 over a panel of nine kinesin motor proteins at a concentration of 5 µM. AZ82 induces multipolar spindle formation in cancer cell lines with high (BT549), but not low (HeLa and MCF-7), numbers of extra chromosomes.  

 

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Description

An inhibitor of KIFC1; binds to the KIFC1/microtubule complex and inhibits its microtubule-stimulated activity (IC50 = 300 nM) in an ATP-competitive (Ki = 43 nM) and microtubule-noncompetitive manner; does not inhibit basal KIFC1 activity at a concentration of 100 µM; selective for KIFC1 over a panel of nine kinesin motor proteins at a concentration of 5 µM; AZ82 preferentially induces multipolar spindle formation in cancer cell lines with high numbers of extra chromosomes

Formal name: αR-[[(5-methyl-4-propyl-2-thienyl)carbonyl]amino]-N-(3R)-3-pyrrolidinyl-6-[3-(trifluoromethoxy)phenyl]-3-pyridinepropanamide

Synonyms: 

Molecular weight: 560.6

CAS: 1449578-65-7

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Microtubule Dynamics||Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer|Cell Cycle|G2/M

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