Acacetin (Synonyms: 5,7-Dihydroxy-4'-methoxyflavone)

Name: Acacetin
Brand: MedChemExpress
SKU: HY-N0451
Rating: 5.0 (8 reviews)

Cat. No.: HY-N0451 Purity: 99.83%: FAQs
Data Sheet SDS COA Handling Instructions

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Acacetin (5,7-Dihydroxy-4'-methoxyflavone) is an orally active flavonoid derived from Dendranthema morifolium. Acacetin docks in the ATP binding pocket of PI3Kγ. Acacetin causes cell cycle arrest and induces apoptosis and autophagy in cancer cells. Acacetin has potent anti-cancer and anti-inflammatory activity and has the potential for pain-related diseases research.

For research use only. We do not sell to patients.

Acacetin Chemical Structure

CAS No. : 480-44-4

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 40	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 40	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 36	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 55	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 94	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 141	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 212	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Based on 8 publication(s) in Google Scholar

Other Forms of Acacetin:

Acacetin (Standard) Get quote

8 Publications Citing Use of MCE Acacetin

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Biological Activity
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Description

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.4 μg/mL Compound: Acacetin	Cytotoxicity against human A549 cells by SRB assay Cytotoxicity against human A549 cells by SRB assay	[PMID: 31784199]
HCT-15	IC₅₀	0.4 μg/mL Compound: Acacetin	Cytotoxicity against human HCT15 cells by SRB assay Cytotoxicity against human HCT15 cells by SRB assay	[PMID: 31784199]
MOLM-13	IC₅₀	9.1 μM Compound: 28	Cytotoxicity against human MOLM-13 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Cytotoxicity against human MOLM-13 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 33393294]
Monocyte	IC₅₀	22 μM Compound: Acacetin	Inhibition of TNFalpha expression in LPS-stimulated human monocytes treated 30 mins before LPS challenge measured after 14 hrs by ELISA Inhibition of TNFalpha expression in LPS-stimulated human monocytes treated 30 mins before LPS challenge measured after 14 hrs by ELISA	[PMID: 10096854]
MV4-11	IC₅₀	6.8 μM Compound: 28	Cytotoxicity against human MV4-11 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Cytotoxicity against human MV4-11 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 33393294]
Neutrophil	IC₅₀	7 μM Compound: 4d	Inhibition of oxidative burst in PMA-stimulated human neutrophils assessed as inhibition of superoxide anion radical-induced lucigenin oxidation incubated for 5 mins prior to PMA challenge by chemiluminescence assay Inhibition of oxidative burst in PMA-stimulated human neutrophils assessed as inhibition of superoxide anion radical-induced lucigenin oxidation incubated for 5 mins prior to PMA challenge by chemiluminescence assay	[PMID: 23871908]
RAW264.7	IC₅₀	27.7 μM Compound: 27	Inhibition of LPS-stimulated nitric oxide production in mouse RAW264.7 cells by Greiss method Inhibition of LPS-stimulated nitric oxide production in mouse RAW264.7 cells by Greiss method	[PMID: 27955927]
RAW264.7	IC₅₀	5.9 μM Compound: 17	Inhibition of LPS induced NO production in mouse RAW264.7 cells measured after 24 hrs by Griess reagent based assay Inhibition of LPS induced NO production in mouse RAW264.7 cells measured after 24 hrs by Griess reagent based assay	[PMID: 33667099]
RAW264.7	IC₅₀	53.7 μM Compound: 27	Inhibition of LPS/INF-gamma-stimulated nitric oxide production in mouse RAW264.7 cells by Greiss method Inhibition of LPS/INF-gamma-stimulated nitric oxide production in mouse RAW264.7 cells by Greiss method	[PMID: 27955927]
RAW264.7	IC₅₀	6.2 μM Compound: 11	Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as decrease in PGE2 production preincubated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as decrease in PGE2 production preincubated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA	[PMID: 31747281]
RAW264.7	CC₅₀	60.9 μM Compound: 17	Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay	[PMID: 33667099]
SK-MEL-2	IC₅₀	0.4 μg/mL Compound: Acacetin	Cytotoxicity against human SK-MEL-2 cells by SRB assay Cytotoxicity against human SK-MEL-2 cells by SRB assay	[PMID: 31784199]
SK-OV-3	IC₅₀	0.4 μg/mL Compound: Acacetin	Cytotoxicity against human SKOV3 cells by SRB assay Cytotoxicity against human SKOV3 cells by SRB assay	[PMID: 31784199]
XF498	IC₅₀	0.4 μg/mL Compound: Acacetin	Cytotoxicity against human XF498 cells by SRB assay Cytotoxicity against human XF498 cells by SRB assay	[PMID: 31784199]

In Vitro

Acacetin (5,7-Dihydroxy-4'-methoxyflavone; 10-200 μM; 24 hours) decreases cell viabilities in a dose-dependent manner. Acacetin has little effect on human normal glial cell line HEB and non-tumorigenic epithelial cell line MCF-10A^[1].
Acacetin (50-150 μM; 24 hours) causes G2/M cell cycle arrest and induces apoptosis and autophagy^[1].
Acacetin (50-150 μM; 24 hours) leads to decreases in levels of PI3Kγ-p110, p-AKT, p-mTOR, p-p70S6K, and p-ULK in a dose-dependent manner^[1].

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

Cell Viability Assay^[1]

Cell Line:	Breast cancer MCF-7 cells, hepatocellular carcinoma SMMC-7721 cells, lung adenocarcinoma A549 cells, esophageal carcinoma Eca109 cells
Concentration:	10, 20, 40, 60, 80, 100, 150, 200 μM
Incubation Time:	24 hours
Result:	Decreased cancer cell viabilities in a dose-dependent manner. Had IC₅₀ values of 82.75 μM, 103.9 μM, 157.4 μM, 54.7 μM in MDA-MB-231, MCF-7, A549, Eca109 cells, respectively.

Cell Cycle Analysis^[1]

Cell Line:	MDA-MB-231 cells
Concentration:	50, 100, 150 μM
Incubation Time:	24 hours
Result:	Resulted in increase in percentage of cells at G2/M phase and decrease in percentage of cells at G1 and S phase in a dose-dependent manner.

Apoptosis Analysis^[1]

Cell Line:	MDA-MB-231 cells
Concentration:	50, 100, 150 μM
Incubation Time:	24 hours
Result:	Induced apoptosis.

Cell Autophagy Assay^[1]

Cell Line:	MDA-MB-231 cells
Concentration:	50, 100, 150 μM
Incubation Time:	24 hours
Result:	Induced autophagy. Resulted in marked increases in EGFP-LC3 puncta formation and a dose-dependent accumulation of LC3-II.

Western Blot Analysis^[1]

Cell Line:	MDA-MB-231 cells
Concentration:	50, 100, 150 μM
Incubation Time:	24 hours
Result:	Resulted in decrease in levels of Bcl-2 and Bcl-xL and increase in levels of p53. Led to decreases in levels of PI3Kγ-p110, p-AKT, p-mTOR, p-p70S6K, and p-ULK in a dose-dependent manner. Had little or no effect on expression of PI3Kα, PI3Kβ, PI3Kδ, p-ERK, p-p38, and p-JNK.

In Vivo

Acacetin (5,7-Dihydroxy-4'-methoxyflavone; 5, 20 mg/kg/day; orally; for 3 days) significantly suppresses microglial activation in an LPS-induced neuroinflammation mouse model^[2].
Acacetin (25 mg/kg/day; orally; for 3 days) reduces neuronal cell death in an animal model of ischemia^[2].
Acacetin (1.8-56.2 mg/kg/day; ip; single dose) decreases visceral and inflammatory nociception and prevented the formalin-induced oedema^[3].

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

Animal Model:	Male C57BL/6 mice, 7 weeks of age^[2]
Dosage:	5, 20 mg/kg
Administration:	Orally; once a day for 3 days
Result:	Significantly suppressed microglial activation in an LPS-induced (ip; 5mg/kg) neuroinflammation mouse model.

Molecular Weight

284.26

Formula

C₁₆H₁₂O₅

CAS No.

480-44-4

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1C=C(C2=CC=C(OC)C=C2)OC3=CC(O)=CC(O)=C13

Structure Classification

Initial Source

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL (439.74 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	3.5179 mL	17.5895 mL	35.1791 mL
5 mM	0.7036 mL	3.5179 mL	7.0358 mL
10 mM	0.3518 mL	1.7590 mL	3.5179 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Dilution Calculator

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

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.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (7.32 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 5 mg/mL (17.59 mM); Suspended solution; Need ultrasonic
Protocol 2

Add each solvent one by one: 0.5% CMC-Na/saline water
Solubility: 10 mg/mL (35.18 mM); Suspended solution; Need ultrasonic
Protocol 3

Add each solvent one by one: 0.5% CMC/saline water
Solubility: 2.5 mg/mL (8.79 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.83%

Select Batch:

Data Sheet (280 KB) SDS (393 KB)

COA (247 KB) LCMS (97 KB)

Handling Instructions (2659 KB)

References

[1]. Hong-Wei Zhang, et al. Flavonoids inhibit cell proliferation and induce apoptosis and autophagy through downregulation of PI3Kγ mediated PI3K/AKT/mTOR/p70S6K/ULK signaling pathway in human breast cancer cells. Sci Rep. 2018 Jul 26;8(1):11255. [Content Brief]

[2]. Sang Keun Ha, et al. Acacetin attenuates neuroinflammation via regulation the response to LPS stimuli in vitro and in vivo. Neurochem Res. 2012 Jul;37(7):1560-7. [Content Brief]

[3]. A I Carballo-Villalobos, et al. Evidence of mechanism of action of anti-inflammatory/antinociceptive activities of acacetin. Eur J Pain. 2014 Mar;18(3):396-405. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.5179 mL	17.5895 mL	35.1791 mL	87.9477 mL
	5 mM	0.7036 mL	3.5179 mL	7.0358 mL	17.5895 mL
	10 mM	0.3518 mL	1.7590 mL	3.5179 mL	8.7948 mL
	15 mM	0.2345 mL	1.1726 mL	2.3453 mL	5.8632 mL
	20 mM	0.1759 mL	0.8795 mL	1.7590 mL	4.3974 mL
	25 mM	0.1407 mL	0.7036 mL	1.4072 mL	3.5179 mL
	30 mM	0.1173 mL	0.5863 mL	1.1726 mL	2.9316 mL
	40 mM	0.0879 mL	0.4397 mL	0.8795 mL	2.1987 mL
	50 mM	0.0704 mL	0.3518 mL	0.7036 mL	1.7590 mL
	60 mM	0.0586 mL	0.2932 mL	0.5863 mL	1.4658 mL
	80 mM	0.0440 mL	0.2199 mL	0.4397 mL	1.0993 mL
	100 mM	0.0352 mL	0.1759 mL	0.3518 mL	0.8795 mL

Acacetin Related Classifications

Help & FAQs

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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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Acacetin (Synonyms: 5,7-Dihydroxy-4'-methoxyflavone)

Customer Review

Other Forms of Acacetin:

8 Publications Citing Use of MCE Acacetin

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

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Purity & Documentation

References

Customer Review

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Complete Stock Solution Preparation Table

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Acacetin (Synonyms: 5,7-Dihydroxy-4'-methoxyflavone)

Customer Review

Other Forms of Acacetin:

Acacetin Related Antibodies

8 Publications Citing Use of MCE Acacetin

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Purity & Documentation

References

Customer Review

Acacetin Related Antibodies

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Complete Stock Solution Preparation Table

Acacetin Related Classifications

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