Hexamethylquercetagetin
Based on 1 Customer Validation
Hexamethylquercetagetin (Hexa-O-methylquercetagetin; Quercetagetin hexamethyl ether; 3,5,6,7,3',4'-Hexamethoxyflavone) is an orally active NF-κB inhibitor. Hexamethylquercetagetin inhibits NF-κB-derived luciferase activity, reduces phosphorylated p65 and IκBα, Cyclin D1, Bcl-2 and blocks TNFα-induced NF-κB activation. Hexamethylquercetagetin inhibits survival and proliferation of cervical carcinoma cells. Hexamethylquercetagetin suppresses tumor volume and weight in BALB/c nude mouse xenograft models of cervical carcinoma. Hexamethylquercetagetin can be used for the research of cancer, such as cervical carcinoma.
For research use only. We do not sell to patients.
- Purity: 98.0%
- CAS No.: 1251-84-9
- Formula: C21H22O8
- Molecular Weight:402.39
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Biological Activity
|
Bcl-2 |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| Col2 | ED50 |
>20 μg/mL
Compound: 2
|
Cytotoxicity against human Col2 cells
Cytotoxicity against human Col2 cells
|
[PMID: 12828478] |
| HL-60 | IC50 |
20.59 μM
Compound: VII, HexaMF
|
Antiproliferative activity against HL60 after 24 hrs
Antiproliferative activity against HL60 after 24 hrs
|
[PMID: 17391969] |
| HUVEC | ED50 |
>20 μg/mL
Compound: 2
|
Cytotoxicity against HUVEC
Cytotoxicity against HUVEC
|
[PMID: 12828478] |
| KB | ED50 |
>20 μg/mL
Compound: 2
|
Cytotoxicity against human KB cells
Cytotoxicity against human KB cells
|
[PMID: 12828478] |
| LNCaP | ED50 |
>20 μg/mL
Compound: 2
|
Cytotoxicity against human LNCAP cells
Cytotoxicity against human LNCAP cells
|
[PMID: 12828478] |
| Lu1 | ED50 |
>20 μg/mL
Compound: 2
|
Cytotoxicity against human Lu1 cells
Cytotoxicity against human Lu1 cells
|
[PMID: 12828478] |
| TERT-RPE1 | ED50 |
>20 μg/mL
Compound: 2
|
Cytotoxicity against human telomerase reverse transcriptase expressing RPE1 cells
Cytotoxicity against human telomerase reverse transcriptase expressing RPE1 cells
|
[PMID: 12828478] |
Hexamethylquercetagetin (25-100 μM; 24 h) potently suppresses NF-κB-driven luciferase activity in Ca Ski and C-33 A cervical carcinoma cells[2].
Hexamethylquercetagetin (25-100 μM; 24 h) inhibits viability of Ca Ski, C-33 A, HeLa, and SiHa cervical carcinoma cells in a concentration-dependent manner, but does not affect viability of NIH3T3 normal fibroblast cells[2].
Hexamethylquercetagetin (25-100 μM; 24 h) inhibits NF-κB signaling in Ca Ski and C-33 A cervical carcinoma cells by reducing concentration-dependent expression of p-p65, p-IκBα, Cyclin D1, and Bcl-2[2].
Hexamethylquercetagetin (25-100 μM; 4 h pre-incubation) suppresses TNFα-induced NF-κB activation in Ca Ski and C-33 A cervical carcinoma cells, as measured by reduced p-p65 expression[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human cervical carcinoma Ca Ski, C-33 A, HeLa, SiHa cells, normal mouse fibroblast NIH3T3 cells
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Concentration:25, 50, 100 μM
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Incubation Time:24 h
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Result:Significantly inhibited cell viability in a concentration-dependent manner in Ca Ski, C-33 A, HeLa, and SiHa cervical carcinoma cells.
No significant toxicity was observed in NIH3T3 normal fibroblast cells at any tested concentration.
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Cell Line:human cervical carcinoma Ca Ski, C-33 A cells
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Concentration:25, 50, 100 μM
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Incubation Time:24 h
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Result:Downregulated the relative expression of phosphorylated p65 (p-p65) and phosphorylated IκBα (p-IκBα) in both Ca Ski and C-33 A cells in a concentration-dependent manner, with significant reductions at all tested concentrations relative to untreated cells.
Markedly downregulated the NF-κB downstream proteins Cyclin D1 and Bcl-2 in a concentration-dependent manner in both cell lines.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice with Ca Ski cells xenograft[2]
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Dosage:50 mg/kg; 100 mg/kg
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Administration:p.o.; daily; 15 days
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Result:Significantly reduced tumor volume and tumor weight in a concentration-dependent manner compared to vehicle controls.
Significantly downregulated the relative protein expression of phosphorylated NF-κB p65 (p-p65) in tumor tissue compared to vehicle controls, with the 100 mg/kg dose showing greater inhibition than the 50 mg/kg dose.
Chemical Information
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CAS No. 1251-84-9
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Appearance Solid
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Molecular Weight 402.39
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Formula C21H22O8
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Color Off-white to light yellow
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SMILES
O=C1C(OC)=C(C2=CC=C(OC)C(OC)=C2)OC3=CC(OC)=C(OC)C(OC)=C13
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Synonyms
Hexa-O-methylquercetagetin; Quercetagetin hexamethyl ether; 3,5,6,7,3',4'-Hexamethoxyflavone
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 27.5 mg/mL (68.34 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 (protect from light). 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 (protect from light). 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)
Purity & Documentation
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Data Sheet (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
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 (protect from light). 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 | 2.4852 mL | 12.4258 mL | 24.8515 mL | 62.1288 mL |
| 5 mM | 0.4970 mL | 2.4852 mL | 4.9703 mL | 12.4258 mL | |
| 10 mM | 0.2485 mL | 1.2426 mL | 2.4852 mL | 6.2129 mL | |
| 15 mM | 0.1657 mL | 0.8284 mL | 1.6568 mL | 4.1419 mL | |
| 20 mM | 0.1243 mL | 0.6213 mL | 1.2426 mL | 3.1064 mL | |
| 25 mM | 0.0994 mL | 0.4970 mL | 0.9941 mL | 2.4852 mL | |
| 30 mM | 0.0828 mL | 0.4142 mL | 0.8284 mL | 2.0710 mL | |
| 40 mM | 0.0621 mL | 0.3106 mL | 0.6213 mL | 1.5532 mL | |
| 50 mM | 0.0497 mL | 0.2485 mL | 0.4970 mL | 1.2426 mL | |
| 60 mM | 0.0414 mL | 0.2071 mL | 0.4142 mL | 1.0355 mL |