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Poloxin is a non-ATP competitive Polo-like Kinase 1 inhibitor targeting the polo-box domain (IC50: appr 4.8 μM).

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 5 mg | $32 | In Stock | In Stock | |
| 10 mg | $48 | In Stock | In Stock | |
| 25 mg | $98 | In Stock | In Stock | |
| 50 mg | $163 | In Stock | In Stock | |
| 100 mg | $243 | In Stock | In Stock | |
| 200 mg | $359 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $50 | In Stock | In Stock |
| Description | Poloxin is a non-ATP competitive Polo-like Kinase 1 inhibitor targeting the polo-box domain (IC50: appr 4.8 μM). |
| Targets&IC50 | PLK1 (PBD):4.8 μM, PLK2 (PBD):18.7 μM, PLK3 (PBD):53.9 μM |
| In vitro | Poloxin inhibits proliferation in both cell lines with a comparable efficiency through a 72 h period. Poloxin inhibits the polo-box domain (PBD) interaction (apparent IC50: ~4.8 μM). Poloxin (25 μM) causes defects in centrosome integrity, spindle formation, and chromosome alignment in mitosis. Centrosomal fragmentation induced by Poloxin is partially rescued by Kiz T379E. Poloxin (25 μM) activates the mitotic checkpoint, induces apoptosis and inhibits proliferation of MDA-MB-231 cells. Poloxin shows a loose Plk1 PBD specificity with 4-10 times higher IC50 values for Plk2 and Plk3, and does not significantly inhibit other types of phosphopeptide-binding domains such as FHA, WW, and SH2 domains[1][2][3]. |
| In vivo | Poloxin (40 mg/kg) reduces the proliferation of MDA-MB-231 cells. It also suppresses the growth of the tumor nude mice bearing established xenografts of MDA-MB-231[1]. |
| Molecular Weight | 297.35 |
| Formula | C18H19NO3 |
| Cas No. | 321688-88-4 |
| Smiles | CC(C)C1=C\C(=N\OC(=O)c2ccccc2C)C(C)=CC1=O |
| Relative Density. | 1.11 g/cm3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
| Solubility Information | DMSO: 14 mg/mL (47.08 mM), Sonication is recommended. | |||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (3.36 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
| ||||||||||||||||||||||||||
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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