| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg | |||
| Other Sizes |
| Targets |
Wighteone targets HSP90 receptor and downstream signaling pathways in cancer cells. It has been shown to inhibit the proliferation of EGFR L858R/T790M mutant non-small cell lung cancer. As an isoflavone, Wighteone may also interact with estrogen receptors and other signaling molecules involved in cell proliferation and apoptosis. Its antifungal activity suggests additional targets in fungal pathogens. The compound's anti-proliferative effects are mediated through multiple mechanisms involving cell cycle regulation and apoptosis induction.
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|---|---|
| ln Vitro |
Wighteone exhibits potent anti-proliferative effects on human leukemia HL-60 cancer cell lines. It has in vitro cytocidal activity against KB cells. The compound effectively inhibits the proliferation of EGFR L858R/T790M mutant non-small cell lung cancer through downregulation of HSP90 receptor and downstream signaling. It also displays antifungal activity. These activities suggest broad-spectrum anticancer and antimicrobial potential.
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| ln Vivo |
In vivo activity data for Wighteone are limited in the available literature. Based on its potent in vitro anti-proliferative activity against various cancer cell lines, it is anticipated to have potential in vivo antitumor efficacy. However, specific animal studies detailing its therapeutic effects, dosing, and pharmacokinetics are not extensively documented.
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| Enzyme Assay |
The non-cellular enzyme/receptor binding assay for Wighteone would typically involve binding studies to assess its interaction with HSP90. HSP90 binding affinity can be measured using surface plasmon resonance (SPR), isothermal titration calorimetry (ITC), or fluorescence polarization assays. The compound's ability to inhibit HSP90 ATPase activity can be evaluated using a malachite green assay measuring inorganic phosphate release. Alternatively, binding to estrogen receptors or other targets can be assessed using radioligand binding assays.
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| Cell Assay |
In vitro cellular assays for Wighteone typically use cancer cell lines such as HL-60 leukemia cells, KB cells, and EGFR-mutant non-small cell lung cancer cell lines. Cells are treated with various concentrations of the compound for 24-72 hours. Cell proliferation is assessed using MTT, CCK-8, or trypan blue exclusion assays. Apoptosis is detected by Annexin V/PI staining and caspase activity assays. HSP90 and downstream signaling protein expression is analyzed by Western blotting.
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| Animal Protocol |
In vivo animal studies for Wighteone are not extensively documented. Based on its anticancer activity, typical study designs would involve xenograft mouse models bearing human cancer cells such as HL-60 or EGFR-mutant lung cancer cells. Wighteone would be administered orally or intraperitoneally at varying doses. Tumor growth inhibition, body weight changes, and survival rates would be monitored. Tumor tissues would be analyzed for proliferation and apoptosis markers.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Wighteone are not extensively characterized. As an isoflavone with molecular weight 338.36, it is expected to have moderate oral bioavailability. Isoflavones are generally absorbed and undergo enterohepatic circulation. Metabolic pathways likely involve phase I oxidation and phase II conjugation (glucuronidation and sulfation). Specific PK parameters such as half-life, Cmax, and bioavailability are not well documented.
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| Toxicity/Toxicokinetics |
Toxicological data for Wighteone are limited. As a naturally occurring isoflavone, it is generally considered to have low toxicity at moderate doses. However, comprehensive toxicology studies are not available. The compound may cause skin and eye irritation upon contact. Standard laboratory safety precautions should be observed when handling this compound.
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| References | |
| Additional Infomation |
Wighteone belongs to the 7-hydroxyisoflavone class of compounds, with hydroxyl groups substituted at positions 5, 7, and 4', and an isopentenyl group substituted at position 6. It has been isolated from the banyan tree (Ficus mucuso). Wighteone is a plant metabolite and antifungal agent, and its function is related to isoflavones. It has been reported to exist in apple wood (Maclura pomifera), herbaceous wood (Anthyllis hermanniae), and other organisms with relevant data.
Wighteone is a research-grade natural product intended for laboratory use only. It is not approved for clinical use as a therapeutic agent. Its primary applications include studying the anticancer mechanisms of isoflavones, investigating HSP90 inhibition and EGFR mutant cancer therapy, and exploring antifungal activities of natural products. The compound serves as a valuable tool for natural product and cancer research. |
| Molecular Formula |
C20H18O5
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|---|---|
| Molecular Weight |
338.35392
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| Exact Mass |
338.115
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| CAS # |
51225-30-0
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| PubChem CID |
5281814
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
586.1±50.0 °C at 760 mmHg
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| Flash Point |
212.8±23.6 °C
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| Vapour Pressure |
0.0±1.7 mmHg at 25°C
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| Index of Refraction |
1.667
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| LogP |
5.05
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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 |
3
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| Heavy Atom Count |
25
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| Complexity |
554
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
KIMDVVKVNNSHGZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H18O5/c1-11(2)3-8-14-16(22)9-17-18(19(14)23)20(24)15(10-25-17)12-4-6-13(21)7-5-12/h3-7,9-10,21-23H,8H2,1-2H3
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| Chemical Name |
5,7-dihydroxy-3-(4-hydroxyphenyl)-6-(3-methylbut-2-enyl)chromen-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 |
| 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 (~295.55 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.39 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 (7.39 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 (7.39 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 | 2.9555 mL | 14.7776 mL | 29.5552 mL | |
| 5 mM | 0.5911 mL | 2.9555 mL | 5.9110 mL | |
| 10 mM | 0.2956 mL | 1.4778 mL | 2.9555 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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