| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| Other Sizes |
| Targets |
PLK1
Dihydrobaicalein targets Polo-like kinase 1 (PLK1), a serine/threonine protein kinase that plays a critical role in cell cycle regulation and mitosis. The compound also inhibits VRK2 and PLK2. By inhibiting PLK1, Dihydrobaicalein disrupts mitotic progression and induces cell cycle arrest. The compound is a natural product from Scutellaria species. |
|---|---|
| ln Vitro |
In cell-free biochemical assays, Dihydrobaicalein inhibits PLK1 with an IC50 of 6.3 μM. The compound also inhibits VRK2 and PLK2. These activities demonstrate the compound's direct inhibition of these kinase enzymes. The compound's inhibitory activity is typically measured using kinase assays with purified enzymes and peptide substrates.
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| ln Vivo |
In cell-based assays, Dihydrobaicalein inhibits PLK1 activity, leading to disruption of mitotic progression and cell cycle arrest. The compound's effects are evaluated in cancer cell lines by assessing cell proliferation, cell cycle distribution, and apoptosis. As a natural product from Scutellaria species, it may also exhibit antioxidant and other biological activities. The compound can be used to study the role of PLK1 in cancer and other diseases.
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| Enzyme Assay |
The cell-free assay for PLK1 inhibition involves measuring the kinase activity of purified PLK1 enzyme in the presence of the compound. The assay uses a peptide substrate and ATP, and the phosphorylation of the substrate is measured using radioactivity, fluorescence, or luminescence. The IC50 of 6.3 μM is determined from dose-response curves. The compound's selectivity for PLK1 over other kinases can be assessed using kinase profiling assays.
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| Cell Assay |
Cell-based assays for Dihydrobaicalein involve culturing cancer cell lines and treating them with the compound at concentrations ranging from 0.1 to 100 μM. Cells are incubated for 24-72 hours, and cell viability is assessed using MTT or CCK-8 assays. Cell cycle analysis is performed by flow cytometry. Apoptosis is evaluated by Annexin V staining or caspase activity assays. The compound's effects on PLK1 activity and downstream signaling are assessed by Western blotting.
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| Animal Protocol |
There is no established animal experimental protocol for Dihydrobaicalein specifically. As a PLK1 inhibitor with potential anti-cancer activity, the compound could potentially be evaluated in animal models of cancer. Typical studies involve administration of the compound to tumor-bearing mice via intraperitoneal or oral routes. Tumor growth, cell cycle markers, and apoptosis are assessed. The compound's natural product origin may influence its pharmacokinetic properties.
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| ADME/Pharmacokinetics |
Dihydrobaicalein is a natural product with limited pharmacokinetic data available. As a small molecule with a molecular weight of 272.25 g/mol, the compound would be expected to have moderate oral bioavailability and tissue penetration. The compound is soluble in DMSO: 10 mg/mL (36.73 mM). It is typically stored at low temperature: powder at -20°C for 3 years or in solvent at -80°C for 1 year.
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| Toxicity/Toxicokinetics |
Dihydrobaicalein is intended for research use only and lacks established toxicity profiles for therapeutic applications. Standard laboratory safety precautions should be observed when handling this natural product. As a PLK1 inhibitor, the compound may have effects on normal dividing cells as well as cancer cells. The compound is typically stored at low temperature. Standard toxicity studies would be required for therapeutic development.
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| References | |
| Additional Infomation |
Dihydrobaicalein is a type of flavanone compound. It has been reported that Scutellaria baicalensis contains dihydrobaicalein, and relevant data is available for reference.
Dihydrobaicalein is a research-grade natural product supplied for cancer research and kinase inhibition studies. It is not an approved pharmaceutical and has no clinical trial history. The compound is a PLK1 inhibitor with an IC50 of 6.3 μM and also inhibits VRK2 and PLK2. It is a natural product from Scutellaria baicalensis. This product is intended for research use only. |
| Molecular Formula |
C15H12O5
|
|---|---|
| Molecular Weight |
272.25
|
| Exact Mass |
272.068
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| CAS # |
35683-17-1
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| PubChem CID |
9816931
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| Appearance |
White to light yellow solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
595.0±50.0 °C at 760 mmHg
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| Flash Point |
231.7±23.6 °C
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| Vapour Pressure |
0.0±1.7 mmHg at 25°C
|
| Index of Refraction |
1.693
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| LogP |
3.83
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
20
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| Complexity |
365
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
GPDJGLOROGNHJD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H12O5/c16-9-6-11(8-4-2-1-3-5-8)20-12-7-10(17)14(18)15(19)13(9)12/h1-5,7,11,17-19H,6H2
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| Chemical Name |
5,6,7-trihydroxy-2-phenyl-2,3-dihydrochromen-4-one
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6731 mL | 18.3655 mL | 36.7309 mL | |
| 5 mM | 0.7346 mL | 3.6731 mL | 7.3462 mL | |
| 10 mM | 0.3673 mL | 1.8365 mL | 3.6731 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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