3',4'-Dimethoxyflavone
Based on 1 publication(s) in Google Scholar
3',4'-Dimethoxyflavone is a lipophilic flavone, can be isolated from the leaves of Primula veris. 3',4'-Dimethoxyflavone can reduce the synthesis and accumulation of PARP and protect cortical neurones against cell death induced by Parthanatos. 3',4'-Dimethoxyflavone is also an aryl hydrocarbon receptor antagonist in human breast cancer cells. 3',4'-Dimethoxyflavone can promote the proliferation of human hematopoietic stem cells. 3',4'-Dimethoxyflavone has various biological activities, including antioxidant, anti-cancer, anti-inflammatory, anti-atherogenic, hypolipidaemic, and neuroprotective or neurotrophic effects.
For research use only. We do not sell to patients.
- Purity : 98.63%
- CAS No.: 4143-62-8
- Formula: C17H14O4
- Molecular Weight:282.29
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) 3',4'-Dimethoxyflavone
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Biological Activity
Description
IC50 & Target
PARP, Aryl hydrocarbon receptor[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| RAW264.7 | IC50 |
34.54 μM
Compound: 3f
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Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-stimulated NO production by ELISA
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-stimulated NO production by ELISA
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[PMID: 28408221] |
| RAW264.7 | IC50 |
39.68 μM
Compound: 3f
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Cytotoxicity against mouse RAW264.7 cells by MTT assay
Cytotoxicity against mouse RAW264.7 cells by MTT assay
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[PMID: 28408221] |
| RAW264.7 | IC50 |
6.46 μM
Compound: 3f
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Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-stimulated PGE2 production by ELISA
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-stimulated PGE2 production by ELISA
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[PMID: 28408221] |
| RBL-2H3 | IC50 |
>500 μM
Compound: 12
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Antihistaminic activity in rat RBL2H3 cells assessed as inhibition of DNP-BSA-induced beta-hexosaminidase release preincubated for 10 mins before DNP-BSA challenge
Antihistaminic activity in rat RBL2H3 cells assessed as inhibition of DNP-BSA-induced beta-hexosaminidase release preincubated for 10 mins before DNP-BSA challenge
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[PMID: 14510616] |
In Vitro
3',4'-Dimethoxyflavone (10 and 20 μM) has protection against the reduction in SH-SY5Y viability induced by Methylnitronitrosoguanidine (MNNG) (HY-128612)[2].
3',4'-Dimethoxyflavone (6.25-25 μM) decreases the levels of PAR induced by MNNG in HeLa cells[2].
3',4'-Dimethoxyflavone (12.5, 25, 50 and 100 μM; 15-20 h) reduces cortical neuronal death induced by exposure to NMDA (HY-17551)[2].
3',4'-Dimethoxyflavone (0.1-10 μM; 24 h) exhibits significant inhibition of 2,3,7,8-Tetrachlorodibenzo-p-dioxin (TCDD)-induced EROD activity in MCF-7 and T47D cells[3].
3',4'-Dimethoxyflavone inhibits AhR-dependent CYP1A1 induction and AhR-mediated inhibition of estrogen-induced gene expression in T47D and MCF-7 breast cancer cells[3].
3′,4′-Dimethoxyflavone (2.5 μM; 7 days) promotes the proliferation of human hematopoietic stem cells[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:Primary cortical neurones (isolated from fetal CD1 mice, incubated with NMDA)
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Concentration:12.5, 25, 50 and 100 μM
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Incubation Time:15-20 h
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Result:Reduced concentration-dependently neuronal death induced by exposure to NMDA.
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Cell Line:CD34+ cells
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Concentration:2.5 μM
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Incubation Time:7 days
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Result:Induced a significantly higher amplification of the CD34+ population under normoxia.
Chemical Information
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CAS No. 4143-62-8
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Appearance Solid
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Molecular Weight 282.29
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Formula C17H14O4
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Color White to light yellow
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SMILES
O=C1C=C(C2=CC=C(OC)C(OC)=C2)OC3=CC=CC=C13
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Structure Classification
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Front Oncol
Cancer Associated Fibroblasts Promote Renal Cancer Progression Through a TDO/Kyn/AhR Dependent Signaling Pathway. [Abstract]2021 Mar 25:11:628821. PMID: 33842334
Solvent & Solubility
In Vitro:
DMSO : ≥ 50 mg/mL (177.12 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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)
In Vivo:
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 (8.86 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.
In Vivo Dissolution Calculator
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.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Mammalian live/dead viability and cytotoxicity staining
Live/dead viability and cytotoxicity staining assays are based on the simultaneous detection of intracellular esterase activity in metabolically active (viable) cells and membrane integrity loss in non-viable cells. In commonly used dual-staining approaches, membrane-permeant fluorogenic substrates are converted by intracellular esterases into fluorescent products in live cells, while impermeant DNA-binding dyes selectively enter cells with compromised plasma membranes and label nucleic acids in dead or dying cells, enabling discrimination between viable and non-viable populations by fluorescence microscopy or flow cytometry.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Korean - KR (479 KB)
- Portuguese - PT (479 KB)
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Handling Instructions (2659 KB)
References
[1]. Budzianowski J, et al. Lipophilic flavones of Primula veris L. from field cultivation and in vitro cultures. Phytochemistry. 2005 May;66(9):1033-9. [Content Brief]
[2]. Fatokun AA, et al. Identification through high-throughput screening of 4'-methoxyflavone and 3',4'-dimethoxyflavone as novel neuroprotective inhibitors of parthanatos. Br J Pharmacol. 2013 Jul;169(6):1263-78. [Content Brief]
[3]. Lee JE, et al. 3',4'-dimethoxyflavone as an aryl hydrocarbon receptor antagonist in human breast cancer cells. Toxicol Sci. 2000 Dec;58(2):235-42. [Content Brief]
[4]. Kaur K, et al. 3',4'-Dimethoxyflavone and valproic acid promotes the proliferation of human hematopoietic stem cells. Stem Cell Res Ther. 2013 May 24;4(3):60. [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 | 3.5425 mL | 17.7123 mL | 35.4246 mL | 88.5614 mL |
| 5 mM | 0.7085 mL | 3.5425 mL | 7.0849 mL | 17.7123 mL | |
| 10 mM | 0.3542 mL | 1.7712 mL | 3.5425 mL | 8.8561 mL | |
| 15 mM | 0.2362 mL | 1.1808 mL | 2.3616 mL | 5.9041 mL | |
| 20 mM | 0.1771 mL | 0.8856 mL | 1.7712 mL | 4.4281 mL | |
| 25 mM | 0.1417 mL | 0.7085 mL | 1.4170 mL | 3.5425 mL | |
| 30 mM | 0.1181 mL | 0.5904 mL | 1.1808 mL | 2.9520 mL | |
| 40 mM | 0.0886 mL | 0.4428 mL | 0.8856 mL | 2.2140 mL | |
| 50 mM | 0.0708 mL | 0.3542 mL | 0.7085 mL | 1.7712 mL | |
| 60 mM | 0.0590 mL | 0.2952 mL | 0.5904 mL | 1.4760 mL | |
| 80 mM | 0.0443 mL | 0.2214 mL | 0.4428 mL | 1.1070 mL | |
| 100 mM | 0.0354 mL | 0.1771 mL | 0.3542 mL | 0.8856 mL |