| Size | Price | Stock | Qty |
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| 10mg |
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| Targets |
Poloxin targets the polo-box domain (PBD) of polo-like kinase 1 (Plk1). Plk1 is a serine/threonine kinase that plays a critical role in cell division, including centrosome maturation, spindle formation, and cytokinesis. The PBD is a protein-protein interaction domain that is essential for Plk1 localization and function. Poloxin is the first reported small-molecule inhibitor specifically targeting the Plk1 PBD.
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| ln Vitro |
Defects in spindle formation, chromosomal alignment, and centrosome integrity occur during mitosis when poloxyxin (25 μM) is administered. Kiz T379E partially restores centrosome fragmentation caused by poloxin. MDA-MB-231 cell growth is inhibited, apoptosis is induced, and mitotic checkpoints are activated by poloxin (25 μM) [1]. Within 72 hours, poloxin effectively stopped both cell lines from proliferating [2]. With an apparent IC50 of about 4.8 μM, poloxin inhibits interactions with the polo-box domain (PBD). With 4–10 times higher IC50 values for Plk2 and Plk3, poloxin shows a loose specificity for the Plk1 PBD. It does not appreciably inhibit other types of phosphopeptide-binding domains, such as FHA, WW, and SH2 domains [3].
Poloxin demonstrates potent inhibition of the Plk1 PBD interaction with an apparent IC50 of ∼4.8 μM. It shows less potent inhibition for Plk2 PBD and Plk3 PBD, indicating some selectivity. In cell-based assays, it induces centrosome fragmentation, abnormal spindle formation, and chromosome misalignment. It activates the mitotic checkpoint, induces apoptosis, and inhibits proliferation of cancer cells. It inhibits proliferation in both cell lines with comparable efficiency through a 72-hour period. |
| ln Vivo |
Poloxin (40 mg/kg) suppresses the growth of tumor-bearing nude mice with established MDA-MB-231 xenografts and decreases the proliferation of MDA-MB-231 cells [1].
Poloxin has been studied in vivo for its anticancer activity. As a Plk1 PBD inhibitor, it induces mitotic arrest and apoptosis in cancer cells. Its ability to inhibit Plk1 function has been demonstrated in preclinical models. It is a valuable tool in cancer research for studying Plk1 biology and validating it as a therapeutic target. Detailed in vivo efficacy data are limited in publicly available sources. |
| Enzyme Assay |
Plk1 PBD binding assays are performed using recombinant Plk1 PBD protein and a fluorescently labeled phosphopeptide substrate representing the optimal Plk1 binding motif. The assay measures the displacement of the labeled peptide by test compounds, with fluorescence polarization or TR-FRET used to quantify binding affinity. Compounds are serially diluted in assay buffer (50 mM HEPES pH 7.5, 150 mM NaCl, 0.1% BSA, 0.01% Triton X-100) and incubated with Plk1 PBD and labeled peptide for 1-2 hours at room temperature. IC50 values are determined by non-linear regression analysis. Each concentration is tested in duplicate.
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| Cell Assay |
Cellular Plk1 inhibition is evaluated in cancer cell lines (e.g., HeLa, MDA-MB-231). Cells are cultured in appropriate media at 37°C with 5% CO2 and treated with Poloxin at various concentrations (1-50 μM) for 24-72 hours. Plk1 localization is assessed by immunofluorescence microscopy. Mitotic arrest is evaluated by flow cytometry (phospho-histone H3 staining) and by microscopy for mitotic index. Apoptosis is assessed by Annexin V/PI staining and caspase-3/7 activity assays. Cell viability and proliferation are assessed using MTT or CellTiter-Glo assays. Each experiment includes vehicle controls.
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| Animal Protocol |
In vivo efficacy is evaluated in mouse xenograft models using cancer cell lines (e.g., MDA-MB-231). Poloxin is administered intraperitoneally at doses determined by preclinical studies. Tumor growth is monitored by caliper measurements. At study endpoint, tumors are harvested for histopathological analysis and biochemical assays (Plk1 activity, apoptosis markers, mitotic markers). Body weight and clinical signs are monitored throughout the study. Sample sizes typically range from 6-10 animals per group.
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| ADME/Pharmacokinetics |
Poloxin has a molecular weight of 297.35 g/mol and a molecular formula of C18H19NO3. Solubility: DMSO: 5 mg/mL (warmed). Storage: powder at -20°C for 3 years; 4°C for 2 years. Bioavailability, half-life, and tissue distribution data are not publicly available. The compound is a research tool for studying Plk1 biology.
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| Toxicity/Toxicokinetics |
Limited toxicology data are available for Poloxin. As a Plk1 inhibitor that induces mitotic arrest and apoptosis, potential toxicities may include effects on normal proliferating tissues. Standard toxicology studies would include acute and subchronic toxicity in rodents, genotoxicity screening, and evaluation of effects on hematopoiesis and gastrointestinal tract. No clinical trials have been reported for this compound. The compound is intended for research use only.
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| References | |
| Additional Infomation |
Poloxin is also known as 2-methyl-5-(1-methylethyl)-2,5-cyclohexadiene-1,4-dione 1-[O-(2-methylbenzoyl)oxime]. It is the first reported small-molecule inhibitor targeting the Plk1 PBD. It induces centrosome fragmentation, mitotic arrest, and apoptosis. It is a valuable tool in cancer research. No clinical trials or regulatory approvals have been reported. The compound is for research use only.
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| Molecular Formula |
C18H19NO3
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| Molecular Weight |
297.34836
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| Exact Mass |
297.136
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| CAS # |
321688-88-4
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| PubChem CID |
9613592
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.619
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
22
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| Complexity |
555
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC=CC=C1C(=O)O/N=C\2/C=C(C(=O)C=C2C)C(C)C
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| InChi Key |
CMOJHDQJJPIVEC-MNDPQUGUSA-N
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| 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/b19-16-
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| Chemical Name |
[(Z)-(2-methyl-4-oxo-5-propan-2-ylcyclohexa-2,5-dien-1-ylidene)amino] 2-methylbenzoate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~14.29 mg/mL (~48.06 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.43 mg/mL (4.81 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 14.3 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.43 mg/mL (4.81 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 14.3 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3630 mL | 16.8152 mL | 33.6304 mL | |
| 5 mM | 0.6726 mL | 3.3630 mL | 6.7261 mL | |
| 10 mM | 0.3363 mL | 1.6815 mL | 3.3630 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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