An inhibitor of KIFC1
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AZ82

Item No. 21898

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
αR-[[(5-methyl-4-propyl-2-thienyl)carbonyl]amino]-N-(3R)-3-pyrrolidinyl-6-[3-(trifluoromethoxy)phenyl]-3-pyridinepropanamide
CAS Number
1449578-65-7
Molecular Formula
C28H31F3N4O3S
Formula Weight
560.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 20 mg/mlEthanol: 20 mg/mlEthanol:PBS (pH 7.2) (1:3): 0.25 mg/ml
λmax
252, 282 nm
SMILES
O=C(N[C@@H]1CCNC1)[C@H](NC(C2=CC(CCC)=C(C)S2)=O)CC3=CC=C(C4=CC(OC(F)(F)F)=CC=C4)N=C3
InChi Code
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
InChi Key
PMTLKNOARSHUJB-ZJSXRUAMSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $42

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    5 mg

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    10 mg

    $343

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    25 mg

    $653

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    Cayman Chemical
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    Product Description

    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.1 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.2 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Godinho, S.A., and Pellman, D. Causes and consequences of centrosome abnormalities in cancer. Philos. Trans. R. Soc. Lond. B Biol. Sci. 369(1650), 20130467 (2014).

    2. Wu, J., Mikule, K., Wang, W., et al. Discovery and mechanistic study of a small molecule inhibitor for motor protein KIFC1. ACS Chem. Biol. 8(10), 2201-2208 (2013).