Isosilybin A
Based on 2 publication(s) in Google Scholar
Isosilybin A is a PPARγ agonist that can be isolated from silymarin. Isosilybin A activates extrinsic and intrinsic pathways of apoptosis through targeting of the Akt-NF-kB-AR axis. Isosilybin A can relieve the inflammatory response in the rosacea model via inhibiting Erk and p38 signaling pathways and M1 macrophage polarization, with its targets related to RELA and VEGFA. Isosilybin A has anti-prostate cancer (PCA) activity[1][2][3].
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- Purity: 99.63%
- CAS No.: 142796-21-2
- 화학식: C25H22O10
- 분자량:482.44
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Isosilybin A
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| B16-4A5 | IC50 |
10 μM
Compound: 7
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Inhibition of theophylline-stimulated melanogenesis in mouse B16-4A5 cells after 72 hrs
Inhibition of theophylline-stimulated melanogenesis in mouse B16-4A5 cells after 72 hrs
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[PMID: 20189399] |
| Huh-7 | IC50 |
80 μM
Compound: 5
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Cytotoxicity against human Huh7.5.1 cells after 72 hrs
Cytotoxicity against human Huh7.5.1 cells after 72 hrs
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[PMID: 23673225] |
Isosilybin A (25-200 μM) alleviates inflammation in the LL37 amide (HY-P4744)-induced HaCaT cell inflammation model via inhibiting Erk, p38 and NF-κB signaling pathways[1].
Isosilybin A (25-200 μM, 6-30 h) inhibits the polarization of M1 macrophages in the LL37-induced THP-1 cells[1].
Isosilybin A (50-100 μM) renders RELA and VEGFA resistant to protease cleavage, but has no significant effect on KDR degradation[1].
Isosilybin A (30 μM) significantly activates PPARγ in HEK-293 cells are co-transfected with a plasmid encoding full-length human PPARγ[2].
Isosilybin A (10-180 μM, 24-48 h) induces apoptotic death by activating extrinsic and intrinsic pathways in human PCA 22Rv1, LAPC4 and LNCaP cells[3].
Isosilybin A (10-180 μM, 24-48 h) decreases phospho- and total Akt, nuclear levels of p50 and p65 in human PCA 22Rv1, LAPC4 and LNCaP cells[3].
Isosilybin A (90-180 μM, 24-48 h) decreases AR and PSA level in human PCA 22Rv1, LAPC4 and LNCaP cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HaCaT cells and THP-1 cells
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Concentration:25, 50, 100, 200 μM
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Incubation Time:6, 12, 24, 30 h
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Result:Showed certain cytotoxicity in HaCaT cells at 200 μM and THP-1 cells at 100 μM.
Showed no obvious difference in cell viability at low concentrations in HaCaT cells (25, 50, and 100 μM) and in THP-1 cells (12.5, 25, and 50 μM).
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Cell Line:LL37-induced HaCaT cells and THP-1 cells
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Concentration:100 μM
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Incubation Time:/
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Result:Reduced the expression of inflammatory factors and chemokines, including IL1A, IL1B, IL6, CCL2 and CCL20.
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Cell Line:22Rv1, LAPC4 and LNCaP cells
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Concentration:10, 30, 60, 90, 120, 150, 180 μM
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Incubation Time:24, 48 h
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Result:Increased the level of cPARP, DR5, cleaved caspase 8,cleaved caspase 9 and 3.
Decreased the phosphorylation of Bcl2 at the Serine-70 site along with a slight decrease in the total level of Bcl2.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:LL37-induced rosacea-like mice model BALB/c female mice(6-8 weeks old)[1].
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Dosage:1% (50 μL)
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Administration:Topical delivery twice a day for 60 h
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Result:Showed lower severity of skin erythema and smaller redness.
Reduced the infiltrated inflammatory cells.
Reduced the number of F4/80+ macrophages and IL-1β+ cells.
Inhibited the the expression of inflammatory factors and associated chemokines, including IL-1β, IL-6, and Nlrp3.
Chemical Information
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CAS No. 142796-21-2
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Appearance Solid
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분자량 482.44
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화학식 C25H22O10
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Color White to off-white
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SMILES
O=C1[C@H](O)[C@@H](C2=CC=C(O[C@H](C3=CC=C(O)C(OC)=C3)[C@@H](CO)O4)C4=C2)OC5=CC(O)=CC(O)=C15
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Structure Classification
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Int Immunopharmacol
Isosilybin A exhibits anti-inflammatory properties in rosacea by inhibiting MAPK pathway and M1 macrophage polarization. [Abstract]2024 Oct 14;143(Pt 1):113323. PMID: 39405940 -
Chem Biol Interact
Isosilybin regulates lipogenesis and fatty acid oxidation via the AMPK/SREBP-1c/PPARα pathway. [Abstract]2022 Dec 1:368:110250. PMID: 36347319
용액&용해도
DMSO : 100 mg/mL (207.28 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.18 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.18 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Wu CC, et al. Isosilybin A exhibits anti-inflammatory properties in rosacea by inhibiting MAPK pathway and M1 macrophage polarization. Int Immunopharmacol. 2024 Dec 25;143(Pt 1):113323. [Content Brief]
[2]. Pferschy-Wenzig EM, et al. Identification of isosilybin a from milk thistle seeds as an agonist of peroxisome proliferator-activated receptor gamma. J Nat Prod. 2014 Apr 25;77(4):842-7. [Content Brief]
[3]. Deep G, et al. Isosilybin A induces apoptosis in human prostate cancer cells via targeting Akt, NF-κB, and androgen receptor signaling. Mol Carcinog. 2010 Oct;49(10):902-12. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0728 mL | 10.3640 mL | 20.7280 mL | 51.8199 mL |
| 5 mM | 0.4146 mL | 2.0728 mL | 4.1456 mL | 10.3640 mL | |
| 10 mM | 0.2073 mL | 1.0364 mL | 2.0728 mL | 5.1820 mL | |
| 15 mM | 0.1382 mL | 0.6909 mL | 1.3819 mL | 3.4547 mL | |
| 20 mM | 0.1036 mL | 0.5182 mL | 1.0364 mL | 2.5910 mL | |
| 25 mM | 0.0829 mL | 0.4146 mL | 0.8291 mL | 2.0728 mL | |
| 30 mM | 0.0691 mL | 0.3455 mL | 0.6909 mL | 1.7273 mL | |
| 40 mM | 0.0518 mL | 0.2591 mL | 0.5182 mL | 1.2955 mL | |
| 50 mM | 0.0415 mL | 0.2073 mL | 0.4146 mL | 1.0364 mL | |
| 60 mM | 0.0345 mL | 0.1727 mL | 0.3455 mL | 0.8637 mL | |
| 80 mM | 0.0259 mL | 0.1295 mL | 0.2591 mL | 0.6477 mL | |
| 100 mM | 0.0207 mL | 0.1036 mL | 0.2073 mL | 0.5182 mL |
Isosilybin A Related Classifications
HY-N7043 Related Classifications
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