| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Targets |
Poloxime targets the polo-box domain (PBD) of polo-like kinase 1 (Plk1). Plk1 is a serine/threonine protein kinase that plays a critical role in mitosis, including centrosome maturation, spindle formation, and cytokinesis. The PBD is a protein-protein interaction domain that is essential for Plk1 localization and function. Poloxime inhibits phosphopeptide binding to the PBD, thereby disrupting Plk1 function.
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| ln Vitro |
The phosphopeptide binding to the polo-box domain (PBD) of polo-like kinase 1 (Plk1) is inhibited by poloxime (100 μM) [2].
Poloxime demonstrates moderate Plk1 inhibitory activity. At 100 μM, it inhibits phosphopeptide binding to the polo-box domain (PBD) of Plk1. It is a non-ATP-competitive inhibitor. Its IC50 for Plk1 inhibition is not as potent as poloxin, but it is a useful tool for studying Plk1 biology. The compound's moderate activity allows for specific modulation of Plk1 function. |
| ln Vivo |
Poloxime is a hydrolysis product of poloxin and is used as a research tool for studying Plk1 function. As a non-ATP-competitive Plk1 PBD inhibitor, it can be used to study the role of Plk1 in cell cycle regulation and cancer. In vivo studies are limited, as it is primarily used as a tool compound. Its moderate activity makes it suitable for specific experimental applications.
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| 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 Poloxime at various concentrations (1-100 μM) for 24-72 hours. Plk1 activity in cell lysates is measured by kinase assays or by assessing Plk1 localization and phosphorylation of downstream targets. Cell viability and proliferation are assessed using MTT or CellTiter-Glo assays. Mitotic arrest and apoptosis are evaluated by flow cytometry and Western blotting for mitotic markers. Each experiment includes known Plk1 inhibitors (e.g., BI-2536, poloxin) as positive controls.
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| Animal Protocol |
In vivo studies with Poloxime are limited as it is primarily a research tool compound. It is a hydrolysis product of poloxin and may be used in studies where its moderate Plk1 inhibitory activity is required. Any in vivo studies would be conducted in mouse xenograft models using cancer cell lines. The compound would be administered intraperitoneally or orally. Tumor growth would be monitored, and tissues collected for analysis. Detailed protocols are not publicly available.
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| ADME/Pharmacokinetics |
Poloxime has a molecular weight of 179.22 g/mol and a molecular formula of C10H13NO2. Purity: typically ≥95-98%. Solubility: DMSO. Storage: typically at -20°C. 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 Poloxime. As a Plk1 inhibitor, potential toxicities may include effects on cell cycle progression in normal tissues. Standard toxicology studies would include acute and subchronic toxicity in rodents, genotoxicity screening, and evaluation of effects on rapidly dividing tissues. No clinical trials have been reported for this compound. The compound is intended for research use only.
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| References | |
| Additional Infomation |
Poloxime is also known as 4-(hydroxyimino)-2-isopropyl-5-methylcyclohexa-2,5-dien-1-one. It is a hydrolysis product of poloxin and a non-ATP-competitive Plk1 inhibitor. It inhibits phosphopeptide binding to the Plk1 PBD. It is used as a research tool for studying Plk1 function. No clinical trials or regulatory approvals have been reported. The compound is for research use only.
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| Molecular Formula |
C10H13NO2
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|---|---|
| Molecular Weight |
179.21
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| Exact Mass |
179.095
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| CAS # |
17302-61-3
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| PubChem CID |
75393
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
1.928
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
13
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| Complexity |
182
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC(=C(C=C1N=O)C(C)C)O
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| InChi Key |
YQVCMSSJMLGWAM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H13NO2/c1-6(2)8-5-9(11-13)7(3)4-10(8)12/h4-6,12H,1-3H3
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| Chemical Name |
5-methyl-4-nitroso-2-propan-2-ylphenol
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| Synonyms |
Nitrosothymol; Poloxime
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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 : ≥ 100 mg/mL (~557.97 mM)
H2O : < 0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (13.95 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 25.0 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: ≥ 2.5 mg/mL (13.95 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (13.95 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.5800 mL | 27.9002 mL | 55.8005 mL | |
| 5 mM | 1.1160 mL | 5.5800 mL | 11.1601 mL | |
| 10 mM | 0.5580 mL | 2.7900 mL | 5.5800 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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