Cat. No.: HY-N0451

Acacetin

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

16 Cited Publications

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Based on 16 publication(s) in Google Scholar

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.

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Pureté: 99.71%
CAS No.: 480-44-4
Formule: C₁₆H₁₂O₅
Masse moléculaire:284.26

Stockage:

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

Acacetin Chemical Structure

CAS No.: 480-44-4

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (16)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	4 x 10^-1μg/mL Compound: 39	Inhibition of EGFR in human A431 cells Inhibition of EGFR in human A431 cells	[PMID: 1479375]
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]
KB	ED₅₀	>100 μg/mL Compound: NSC-76061	Cytotoxicity against human KB cells Cytotoxicity against human KB cells	[PMID: 469554]
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	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]
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]
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.

Chemical Information

CAS No. 480-44-4
Appearance Solid
Masse moléculaire 284.26
Formule C₁₆H₁₂O₅
Color Light yellow to yellow
SMILES

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

5,7-Dihydroxy-4'-methoxyflavone
Structure Classification
- Flavonoids
- Flavones
- Phenols
- Polyphenols
Initial Source
- Endogenous metabolite
- Human Gut Microbiota Metabolites
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Publications (16)

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Journal Impact Factor

Acta Pharm Sin B

Chrysin serves as a novel inhibitor of DGK α/FAK interaction to suppress the malignancy of esophageal squamous cell carcinoma (ESCC). [Abstract]

2021 Jan;11(1):143-155. PMID: 33532186
Metabolism

Acacetin ameliorates MASLD by inhibiting the Notch1 pathway in hepatocytes and reprogramming macrophage polarization via Keap1-Nrf2-mediated restraint of ferroptosis. [Abstract]

2026 Jun 7:182:156670. PMID: 42259496
Pharmacol Res

Cardamonin retards progression of autosomal dominant polycystic kidney disease via inhibiting renal cyst growth and interstitial fibrosis. [Abstract]

2020 May;155:104751. PMID: 32151678
Food Chem

Effects of sun drying combined with baking processes on the flavor quality of Chongqing Tuocha raw tea. [Abstract]

2025 Dec 30:497:146992. PMID: 41285060
Food Chem

Flavonoid-mediated metabolic underpinning quality variation in red bud-sport pear mutants. [Abstract]

2025 May 31:489:144992. PMID: 40466530
Phytomedicine

Duhuo Jisheng decoction alleviates intervertebral disc degeneration via the acacetin-mediated MAPK1/HMOX1 axis by inhibiting nucleus pulposus cell pyroptosis. [Abstract]

2025 Oct 15:148:157405. PMID: 41135274

Acacetin purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2025 Oct 15:148:157405. [Abstract]

Acacetin (ACA) (10 μM; 24 h) significantly alleviated TBHP-induced pyroptotic alterations in NPCs.

Acacetin purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2025 Oct 15:148:157405. [Abstract]

Acacetin (ACA) (10 μM; 24 h) significantly inhibited TBHP-induced NPC programmed cell death.

Acacetin purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2025 Oct 15:148:157405. [Abstract]

Acacetin (ACA) (10 μM; 24 h) significantly reduced ROS production in NPCs exposed to TBHP.

Acacetin purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2025 Oct 15:148:157405. [Abstract]

Acacetin (ACA) (10 μM; 24 h) downregulated the expression of pyroptosis-related proteins in NPCs exposed to TBHP.

Acacetin purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2025 Oct 15:148:157405. [Abstract]

Acacetin (ACA) (10 μM; 24 h) effectively restored the reduced mitochondrial membrane potential in NPCs induced by TBHP.
EMBO Rep

CDK inhibitor Palbociclib targets STING to alleviate autoinflammation. [Abstract]

2022 Jun 7;23(6):e53932. PMID: 35403787
Int J Mol Sci

Elucidating the Mechanisms of Chrysanthemum Action on Atopic Dermatitis via Network Pharmacology and Machine Learning. [Abstract]

2025 Nov 21;26(23):11262. PMID: 41373428
Sci Rep

Acacetin inhibited non-small-cell lung cancer (NSCLC) cell growth via upregulating miR-34a in vitro and in vivo. [Abstract]

2024 Jan 29;14(1):2348. PMID: 38287075
Heliyon

Mechanism of acacetin regulating hepatic stellate cell apoptosis based on network pharmacology and experimental verification. [Abstract]

2024 Mar 25;10(7):e28693. PMID: 38571642
Chem Biol Drug Des

Acacetin Attenuates Heatstroke-Induced Acute Liver Injury by Targeting the c-Jun/PTGS2 Pathway. [Abstract]

2026 May;107(5):e70308. PMID: 42068089
Neurogastroenterol Motil

Acacetin Alleviates Loperamide-Induced Functional Constipation by Inhibiting P53-Mediated Apoptosis in Colonic Epithelial Cells. [Abstract]

2026 Apr;38(4):e70298. PMID: 41913080
World J Gastrointest Oncol

Effect of acacetin on inhibition of apoptosis in Helicobacter pylori-infected gastric epithelial cell line. [Abstract]

2024 Aug 15;16(8):3624-3634. PMID: 39171164
Future Microbiol

Characterization of the sortase A from Lactobacillus acidophilus ATCC 4356 involved in adherence to intestinal cells. [Abstract]

2020 May;15:485-496. PMID: 32476478
Biol Pharm Bull

Regioselective Glucuronidation of Flavones at C5, C7, and C4' Positions in Human Liver and Intestinal Microsomes: Comparison among Apigenin, Acacetin, and Genkwanin. [Abstract]

2022;45(8):1116-1123. PMID: 35908893
SSRN

2025 May 7.

Solvant et solubilité

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Working Solution

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (280 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

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

16 Cited Publications

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Acacetin

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Publications Citing Use of MedChemExpress (MCE) Acacetin

Activité biologique

Chemical Information

Publications (16)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Acacetin Related Classifications

HY-N0451 Related Classifications