| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| Other Sizes |
| Targets |
Lupiwighteone targets the PI3K/Akt/mTOR signaling pathway, which is frequently dysregulated in cancer. By inhibiting this pathway, it induces apoptosis in cancer cells. It also has antioxidant, antibacterial, and anti-angiogenic activities. Its anticancer effects have been demonstrated in breast cancer, prostate cancer, and neuroblastoma cells.
|
|---|---|
| ln Vitro |
Lupiwighteone (2-100 μM; 72 hours) demonstrates cytotoxicity against many cell lines, with IC50s of 23.7 μM and 21 μM, respectively, against DU-145 and SGC-7901 cells [2]. In 48 hours, lupiwighteone (20–60 μM) causes cell cycle arrest in DU-145 cells [2]. In 48 hours, lupiwighteone (20–60 μM) causes apoptosis [2]. The expression of cell cycle-related proteins in DU-145 cells is lowered in a dose-dependent manner by lupiwighteone (20–60 μM; 48 hours) [2]. A dose-dependent increase in ROS generation is induced by lupiwighteone (20–60 μM; 48 hours) [2]. Inducing mitochondria-based intrinsic apoptosis in DU-145 cells, lupiwighteone up-regulates cytochrome c and caspase-3, cleaves PARP-1, and down-regulates p-Akt/Akt ratio and VEGF expression [2].
Lupiwighteone exhibits potent in vitro anticancer activity. It induces caspase-dependent and -independent apoptosis in human breast cancer cells by inhibiting the PI3K/Akt/mTOR pathway. It has cytotoxic, apoptotic, and antiangiogenic activities in DU-145 prostate cancer cells and anticancer and cancer preventive effects on SH-SY5Y neuroblastoma cells. These in vitro activities confirm its potential as an anticancer agent. |
| ln Vivo |
In vivo, lupiwighteone has demonstrated anticancer activity in preclinical models. Its ability to inhibit the PI3K/Akt/mTOR pathway and induce apoptosis makes it a promising candidate for cancer therapy. Its anti-angiogenic activity may also contribute to its antitumor effects. Further in vivo studies are needed to fully characterize its therapeutic potential.
|
| Enzyme Assay |
In vitro assays for lupiwighteone involve measuring its effects on cancer cell lines. Cells are treated with the compound at various concentrations, and cell proliferation is measured using MTT or CellTiter-Glo assays. Apoptosis is assessed by Annexin V staining, caspase activity assays, or PARP cleavage. PI3K/Akt/mTOR pathway activity is assessed by Western blot. Anti-angiogenic activity is assessed in HUVEC cells.
|
| Cell Assay |
Cell viability assay[2]
Cell Types: DU-145 cells, C4-2 cells, SGC-7901 cells, Hela cells, HUVEC, MCF-7 cells, CNE cells, Vero Tested Concentrations: 2 μM, 5 μM, 25 μM, 50 μM, 100 μM Incubation Duration: 72 hrs (hours) Experimental Results: Inhibitory effect on the survival of various cancer cell lines and HUVEC Cell cycle analysis [2] Cell Types: DU-145 Cell Tested Concentrations: 20 μM, 40 μM, 60 μM Incubation Duration: 48 hour Experimental Results: Induction of cell cycle arrest. Apoptosis analysis[2] Cell Types: DU-145 Cell Tested Concentrations: 20 μM, 40 μM, 60 μM Incubation Duration: 48 hrs (hours) Experimental Results: Induction of apoptosis. Western Blot Analysis [2] Cell Types: DU-145 Cell Tested Concentrations: 20 μM, 40 μM, 60 μM Incubation Duration: 48 hrs (hours) Experimental Results: CDK1, 2, 4, 6, cyclinD1 and cyclinB1 protein expression diminished in a dose-dependent manner. In vitro cellular assays for lupiwighteone are conducted in various cancer cell lines, including breast cancer, prostate cancer (DU-145), and neuroblastoma (SH-SY5Y) cells. Cells are treated with the compound, and cell viability, apoptosis, and signaling pathway activity are measured. These assays characterize the compound's anticancer activity and mechanism of action. |
| Animal Protocol |
In vivo animal experiments with lupiwighteone are conducted in mouse xenograft models of cancer. Tumor-bearing mice are administered lupiwighteone at various doses. Tumor growth is monitored, and tumor tissues are harvested for analysis of apoptosis markers and PI3K/Akt/mTOR pathway activity. Anti-angiogenic effects are assessed by measuring microvessel density.
|
| ADME/Pharmacokinetics |
Pharmacokinetic data for lupiwighteone are limited. It has a molecular weight of 338.35 and a molecular formula of C20H18O5. The compound is soluble in DMSO and is typically stored at -20°C. Its bioavailability and half-life have not been extensively characterized.
|
| Toxicity/Toxicokinetics |
Comprehensive toxicological data for lupiwighteone are limited. The compound is intended for research use only and is not approved for human therapeutic use. Standard laboratory safety precautions should be followed when handling this compound. Further toxicity studies would be required to support any potential clinical development.
|
| References |
|
| Additional Infomation |
Lupiwighteone is a member of the isoflavone family. It has been reported in Cadophora gregata, Glycyrrhiza uralensis, and other organisms with available data.
Lupiwighteone is a naturally occurring isoflavone with antioxidant, antibacterial, and anticancer activities. It induces apoptosis by inhibiting the PI3K/Akt/mTOR pathway. It has anti-angiogenesis potential and has demonstrated anticancer effects in breast, prostate, and neuroblastoma cancer cells. It is isolated from Glycyrrhiza glabra. |
| Molecular Formula |
C20H18O5
|
|---|---|
| Molecular Weight |
338.3539
|
| Exact Mass |
338.115
|
| CAS # |
104691-86-3
|
| PubChem CID |
5317480
|
| Appearance |
Off-white to light yellow solid powder
|
| Density |
1.4±0.1 g/cm3
|
| Boiling Point |
583.5±50.0 °C at 760 mmHg
|
| Melting Point |
133-135℃
|
| Flash Point |
211.8±23.6 °C
|
| Vapour Pressure |
0.0±1.7 mmHg at 25°C
|
| Index of Refraction |
1.667
|
| LogP |
5.05
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
25
|
| Complexity |
554
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
YGCCASGFIOIXIN-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C20H18O5/c1-11(2)3-8-14-16(22)9-17(23)18-19(24)15(10-25-20(14)18)12-4-6-13(21)7-5-12/h3-7,9-10,21-23H,8H2,1-2H3
|
| Chemical Name |
5,7-dihydroxy-3-(4-hydroxyphenyl)-8-(3-methylbut-2-enyl)chromen-4-one
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~295.55 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 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.
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 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 | 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
