| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Targets |
Kushenol A targets multiple enzymes and proteins. It is a confirmed inhibitor of beta-secretase (BACE) and a type of adenosine 3',5'-cyclic monophosphate (cAMP) phosphodiesterase inhibitor. It also shows selective inhibitory activity against alpha-glucosidase and sodium-dependent glucose cotransporter 2 (SGLT2). Furthermore, it is a potent inhibitor of tyrosinase with an IC50 of 1.1 μM.
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| ln Vitro |
At 25 μM, Kushenol A exhibits a high proportion of inhibition of scavenging activity at 93.7%, and an IC50 value of 9.7 ± 0.1 μM against ABTS+ free radical scavenging [1]. Against NSCLC cells, Kushenol A (0-60 μg/ml; 24 hours) demonstrated significant cytotoxicity, with IC50 values of 5.3 μg/ml and 20.5 μg/ml against A549 and NCI-H226 cells, respectively. BEAS-2B cells have an IC50 value of 57.2 μg/ml [3].
In vitro, Kushenol A demonstrates significant enzyme inhibitory activities. It inhibits alpha-glucosidase with an IC50 of 45 μM and a Ki of 6.8 μM. It is a potent tyrosinase inhibitor with an IC50 of 1.1 μM. These activities suggest potential applications in areas like diabetes management and skin whitening. Its inhibition of BACE1 points to possible relevance in Alzheimer's disease research. Studies suggest it can inhibit oxidative stress, downregulate pro-inflammatory cytokines, and suppress tumor cell growth through apoptosis induction and cell cycle regulation. |
| ln Vivo |
Specific in vivo data for Kushenol A are not extensively documented. However, based on its in vitro mechanisms, it is hypothesized to have therapeutic potential for conditions involving inflammation, oxidative stress, and tumor growth. Its inhibitory effects on alpha-glucosidase and SGLT2 suggest it could be beneficial in managing diabetes and metabolic disorders. Further in vivo studies are required to confirm its efficacy and pharmacokinetic profile in animal models.
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| Enzyme Assay |
For in vitro enzyme inhibition assays, the activity of Kushenol A can be evaluated against its targets. For alpha-glucosidase, the enzyme is incubated with a substrate like p-nitrophenyl-α-D-glucopyranoside and varying concentrations of the inhibitor. The release of p-nitrophenol is measured spectrophotometrically at 405 nm to determine the IC50. Tyrosinase activity is measured using L-DOPA as a substrate, with the formation of dopachrome monitored at 475 nm. For BACE1 inhibition, a fluorometric assay using a specific peptide substrate can be employed.
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| Cell Assay |
Cell viability assay [3]
Cell Types: NSCLC cell lines, A549 and NCI-H226 Normal human lung epithelial cells: BEAS-2B Tested Concentrations: 0-60 μg/ml Incubation Duration: 24 hrs (hours) Experimental Results: demonstrated considerable effects on NSCLC cells Cytotoxic effects. For cell-based assays, various cancer cell lines or cell models of inflammation can be used. Cells are cultured and treated with Kushenol A at different concentrations. Cell viability is measured using MTT or CCK-8 assays to assess cytotoxicity and antiproliferative effects. Apoptosis can be evaluated by Annexin V staining and flow cytometry. The compound's anti-inflammatory activity can be assessed by measuring the levels of pro-inflammatory cytokines (e.g., TNF-α, IL-6) in stimulated cells using ELISA. |
| Animal Protocol |
For in vivo studies, Kushenol A is typically administered orally or intraperitoneally in rodent models. To study its anti-inflammatory effects, animal models of acute inflammation (e.g., carrageenan-induced paw edema) can be used. Its anticancer potential can be evaluated in xenograft models where tumor-bearing mice are treated with the compound, and tumor growth is monitored. Blood samples and tissues are collected for further analysis of biomarkers and histopathology.
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| ADME/Pharmacokinetics |
Kushenol A has a molecular weight of 408.49 and a formula of C25H28O5. It is typically stored as a powder at -20°C and is soluble in DMSO. For in vivo administration, it can be formulated in vehicles such as 5% DMSO, 40% PEG300, 5% Tween 80, and 50% saline. Detailed pharmacokinetic parameters, such as half-life and bioavailability, are not publicly available. As a flavonoid, it is expected to have moderate oral bioavailability.
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| Toxicity/Toxicokinetics |
Specific toxicity data for Kushenol A are limited. As a natural compound from Sophora flavescens, which has a history of use in traditional medicine, it is generally considered to have a favorable safety profile. However, comprehensive toxicological studies have not been published. The compound is used for research purposes only and is not intended for human use. Standard laboratory safety precautions should be observed.
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| References |
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| Additional Infomation |
Kushenol A is a flavanone compound. Kushenol A has been found in Sophora flavescens, and relevant data have been reported.
Kushenol A is a research compound with no clinical trial or regulatory approval status. It is a natural product isolated from Sophora flavescens and is used as a research tool to study various enzyme targets. It is commercially available from chemical suppliers for research purposes only. The compound is of interest for its potential applications in diabetes, cancer, and inflammatory diseases. |
| Molecular Formula |
C25H28O5
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|---|---|
| Molecular Weight |
408.4868
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| Exact Mass |
408.193
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| CAS # |
99217-63-7
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| PubChem CID |
44563121
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
581.7±50.0 °C at 760 mmHg
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| Flash Point |
195.8±23.6 °C
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| Vapour Pressure |
0.0±1.7 mmHg at 25°C
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| Index of Refraction |
1.607
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| LogP |
7.24
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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 |
6
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| Heavy Atom Count |
30
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| Complexity |
652
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CC(=CC[C@H](CC1=C2C(=C(C=C1O)O)C(=O)C[C@H](O2)C3=CC=CC=C3O)C(=C)C)C
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| InChi Key |
OGBMVWVBHWHRGD-MWTRTKDXSA-N
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| InChi Code |
InChI=1S/C25H28O5/c1-14(2)9-10-16(15(3)4)11-18-20(27)12-21(28)24-22(29)13-23(30-25(18)24)17-7-5-6-8-19(17)26/h5-9,12,16,23,26-28H,3,10-11,13H2,1-2,4H3/t16-,23+/m1/s1
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| Chemical Name |
(2S)-5,7-dihydroxy-2-(2-hydroxyphenyl)-8-[(2R)-5-methyl-2-prop-1-en-2-ylhex-4-enyl]-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) |
DMSO : ~100 mg/mL (~244.80 mM)
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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 | 2.4480 mL | 12.2402 mL | 24.4804 mL | |
| 5 mM | 0.4896 mL | 2.4480 mL | 4.8961 mL | |
| 10 mM | 0.2448 mL | 1.2240 mL | 2.4480 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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