2. NF-κB Apoptosis
  3. NF-κB IKK Bcl-2 Family
  4. Hexamethylquercetagetin

Hexamethylquercetagetin  (Synonyms: Hexa-O-methylquercetagetin; Quercetagetin hexamethyl ether; 3,5,6,7,3',4'-Hexamethoxyflavone)

Cat. No.: HY-N4308 Purity: 98.0%
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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.

Hexamethylquercetagetin

Hexamethylquercetagetin Chemical Structure

CAS No. : 1251-84-9

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Hexamethylquercetagetin Related Antibodies

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Description

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[1][2].

IC50 & Target[1]

Bcl-2

 

Cellular Effect
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]
In Vitro

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.

Hexamethylquercetagetin Related Antibodies

Cell Viability Assay[2]

Cell Line: human cervical carcinoma Ca Ski, C-33 A, HeLa, SiHa cells, normal mouse fibroblast NIH3T3 cells
Concentration: 25, 50, 100 μM
Incubation Time: 24 h
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.

Western Blot Analysis[2]

Cell Line: human cervical carcinoma Ca Ski, C-33 A cells
Concentration: 25, 50, 100 μM
Incubation Time: 24 h
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.
In Vivo

Hexamethylquercetagetin (50-100 mg/kg; p.o.; daily; 15 days) acts as an NF-κB inhibitor to dose-dependently suppress cervical carcinoma tumor growth in BALB/c nude mice[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c nude mice with Ca Ski cells xenograft[2]
Dosage: 50 mg/kg; 100 mg/kg
Administration: p.o.; daily; 15 days
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.
Molecular Weight

402.39

Formula

C21H22O8
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C1C(OC)=C(C2=CC=C(OC)C(OC)=C2)OC3=CC(OC)=C(OC)C(OC)=C13
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Purity & Documentation
References
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Hexamethylquercetagetin Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Hexamethylquercetagetin1251-84-9Hexa-O-methylquercetagetin Quercetagetin hexamethyl ether 3,5,6,7,3',4'-HexamethoxyflavoneNF-κBIKKBcl-2 FamilyNuclear factor-κBNuclear factor-kappaBIκB kinaseI kappa B kinaseCa SkiHeLaNIH3T3 normal fibroblast cellsIκBαSiHaC-33 Acervical carcinoma cellsTNFαBALB/c nude mouse xenograft modelsInhibitorinhibitorinhibit

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