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

Cat. No.: HY-N4308 Purity: 98.0%: Data Sheet
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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 Chemical Structure

CAS No. : 1251-84-9

Size	Stock	Quantity
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	Get quote
50 mg	Get quote

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Biological Activity
Purity & Documentation
References
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Description

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.

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.

1251-84-9

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)

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.4852 mL	12.4258 mL	24.8515 mL
5 mM	0.4970 mL	2.4852 mL	4.9703 mL
10 mM	0.2485 mL	1.2426 mL	2.4852 mL

View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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Working solution concentration: mg/mL

Purity & Documentation

Purity: 98.0%

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Data Sheet (280 KB) SDS (252 KB)

COA (251 KB) HNMR (162 KB) LCMS (605 KB)

Handling Instructions (2659 KB)

References

[1]. Kupchan S M, et al. Tumor inhibitors. XXXVI. Eupatin and eupatoretin, two cytotoxic flavonols from Eupatorium semiserratum[J]. The Journal of Organic Chemistry, 1969, 34(5): 1460-1463.

[2]. Sun Y, et al. The polymethoxylated flavone hexamethylquercetagetin suppresses NF-κB signaling and inhibits cell survival in cervical carcinoma. Growth Factors. 2023;41(1):1-7. [Content Brief]

Complete Stock Solution Preparation Table

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

Hexamethylquercetagetin Related Classifications

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.

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

Hexamethylquercetagetin Related Antibodies

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View All Bcl-2 Family Isoform Specific Products:

Biological Activity

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References

Customer Review

Hexamethylquercetagetin Related Antibodies

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Complete Stock Solution Preparation Table

Hexamethylquercetagetin Related Classifications

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