An inhibitor of the Plk1 polo-box domain
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Poloxin

Item No. 36018

Technical Information
Formal Name
1-[O-(2-methylbenzoyl)oxime]2-methyl-5-(1-methylethyl)-2,5-cyclohexadiene-1,4-dione
CAS Number
321688-88-4
Molecular Formula
C18H19NO3
Formula Weight
Purity
≥98%
A solid
DMF: 1 mg/mlDMSO: 2 mg/mlEthanol: 1 mg/mlPBS (pH 7.2): insol
λmax
290 nm
SMILES
O=C(C1=C(C)C=CC=C1)ON=C2C=C(C(C)C)C(C=C2C)=O
InChi Code
InChI=1S/C18H19NO3/c1-11(2)15-10-16(13(4)9-17(15)20)19-22-18(21)14-8-6-5-7-12(14)3/h5-11H,1-4H3
InChi Key
CMOJHDQJJPIVEC-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Poloxin is an inhibitor of the polo-like kinase 1 (Plk1) polo-box domain (PBD; apparent IC50 = 4.8 µM).1 It is selective for the Plk1 PBD over Plk2 and Plk3 PBDs (IC50s = 18.7 and 53.9 µM, respectively). Poloxin (5, 10, and 25 µM) induces cell cycle arrest at the G2/M phase, apoptosis, and mislocalization of Plk1 in HeLa cells. It reduces cell proliferation in a panel of 10 cancer cell lines (EC50s = 15-35 µM).2 In vivo, poloxin (40 mg/kg) reduces tumor growth and induces intratumor apoptosis in an MDA-MB-231 breast cancer mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Reindl, W., Yuan, J., Krämer, A., et alInhibition of polo-like kinase 1 by blocking polo-box domain-dependent protein-protein interactions. Chem. Biol. 15(5), 459-466 (2008).

    2. Yuan, J., Sanhaji, M., Krämer, A., et alPolo-box domain inhibitor poloxin activates the spindle assembly checkpoint and inhibits tumor growth in vivo. Am. J. Pathol. 179(4), 2091-2099 (2011).