Cat. No.: HY-16558

Butein

(Synonyms: 2’,3,4,4’-tetrahydroxy Chalcone)

6 Cited Publications

Customer Review

Based on 6 publication(s) in Google Scholar

Butein is a cAMP-specific PDE inhibitor with an IC₅₀ of 10.4 μM for PDE4. Butein is a specific protein tyrosine kinase inhibitor with IC₅₀s of 16 and 65 μM for EGFR and p60^c-src in HepG2 cells. Butein sensitizes HeLa cells to Cisplatin through AKT and ERK/p38 MAPK pathways by targeting FoxO3a. Butein is a SIRT1 activator (STAC).

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

Purity: 99.64%
CAS No.: 487-52-5
Formula: C₁₅H₁₂O₅
Molecular Weight:272.25

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Butein Chemical Structure

CAS No.: 487-52-5

Size

Price

Stock

Quantity

Amount: USD 0.00

* Please select Quantity before adding items.

Top Publications Citing

Use of MCE Products

Antibody-Drug Conjugates

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (6)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

Butein is a cAMP-specific PDE inhibitor with an IC₅₀ of 10.4 μM for PDE4^[1]. Butein is a specific protein tyrosine kinase inhibitor with IC₅₀s of 16 and 65 μM for EGFR and p60^c-src in HepG2 cells^[2]. Butein sensitizes HeLa cells to Cisplatin through AKT and ERK/p38 MAPK pathways by targeting FoxO3a^[3]. Butein is a SIRT1 activator (STAC).

IC₅₀ & Target^[1]

EGFR

16 μM (IC₅₀, in HepG2 cells)

PDE4

10.4 μM (IC₅₀)

All EGFR Isoforms :

All Phosphodiesterase (PDE) Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	>20 μM Compound: 4	Inhibition of TNFalpha induced NF-kappaB activation in human A549 cells by luciferase reporter gene assay Inhibition of TNFalpha induced NF-kappaB activation in human A549 cells by luciferase reporter gene assay	[PMID: 19883086]
BV-2	IC₅₀	10.9 μM Compound: Butein	Antiinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced nitric oxide production pretreated for 1 hr followed by LPS addition and measured after 24 hrs by Griess assay Antiinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced nitric oxide production pretreated for 1 hr followed by LPS addition and measured after 24 hrs by Griess assay	[PMID: 28923363]
BV-2	IC₅₀	10.9 μM Compound: 135	Antiinflammatory activity in mouse BV-2 cells assessed as reduction in LPS-induced NO production incubated for 24 hrs by microplate reader analysis Antiinflammatory activity in mouse BV-2 cells assessed as reduction in LPS-induced NO production incubated for 24 hrs by microplate reader analysis	[PMID: 37683361]
BV-2	IC₅₀	4.3 μM Compound: Butein	Inhibition of LPS-induced NO production in mouse BV2 cells by Griess assay Inhibition of LPS-induced NO production in mouse BV2 cells by Griess assay	[PMID: 27287369]
C2C12	IC₅₀	18.99 μg/mL Compound: 9	Cytotoxicity against mouse C2C12 cells assessed as reduction in cell viability by MTT assay Cytotoxicity against mouse C2C12 cells assessed as reduction in cell viability by MTT assay	[PMID: 33412152]
K562	IC₅₀	38 μM Compound: Butein	Inhibition of NF-kappaB transactivation in TNF-alpha-stimulated human K562 cells preincubated for 2 hrs followed by TNF-alpha challenge measured after 6 hrs by dual luciferase reporter gene assay Inhibition of NF-kappaB transactivation in TNF-alpha-stimulated human K562 cells preincubated for 2 hrs followed by TNF-alpha challenge measured after 6 hrs by dual luciferase reporter gene assay	[PMID: 24775915]
KB	CC₅₀	9.1 μM Compound: 10b	Compound concentration required to reduce the exponential growth of KB cells by 50% Compound concentration required to reduce the exponential growth of KB cells by 50%	[PMID: 9767632]
Macrophage	IC₅₀	43.3 μM Compound: 1	Inhibition of LPS stimulated TNF alpha production in Balb/c mouse peritoneal macrophages measured by ELISA plate reader method Inhibition of LPS stimulated TNF alpha production in Balb/c mouse peritoneal macrophages measured by ELISA plate reader method	[PMID: 32361286]
MT4	CC₅₀	5.3 μM Compound: 10b	Compound concentration required to reduce the exponential growth of MT-4 cells by 50% Compound concentration required to reduce the exponential growth of MT-4 cells by 50%	[PMID: 9767632]
NIH3T3	IC₅₀	>20 μM Compound: 1d	Inhibition of cobalt chloride-induced HIF-1 activation expressed in mouse NIH3T3 cells after 8 hrs by luciferase reporter gene assay Inhibition of cobalt chloride-induced HIF-1 activation expressed in mouse NIH3T3 cells after 8 hrs by luciferase reporter gene assay	[PMID: 21112783]
RAW264.7	IC₅₀	35.1 μM Compound: 11	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess assay Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess assay	[PMID: 23743282]
RAW264.7	IC₅₀	5.3 μM Compound: Butein	Inhibition of LPS-induced NO production in mouse RAW264.7 cells by Griess assay Inhibition of LPS-induced NO production in mouse RAW264.7 cells by Griess assay	[PMID: 27287369]
RBL-1	IC₅₀	0.0046 μM Compound: 11	Inhibition of 5-lipoxygenase in rat RBL1 cells Inhibition of 5-lipoxygenase in rat RBL1 cells	10.1007/s00044-013-0745-7
RBL-1	IC₅₀	0.0046 μM Compound: 11	Inhibition of cyclooxygenase in rat RBL1 cells Inhibition of cyclooxygenase in rat RBL1 cells	10.1007/s00044-013-0745-7
RBL-1	IC₅₀	0.0046 μM Compound: 12	In vitro inhibition against 5-lipoxygenase in RBL-1 cells was determined In vitro inhibition against 5-lipoxygenase in RBL-1 cells was determined	[PMID: 8254620]

In Vitro

Butein potently inhibits cAMP-specific phosphodiesterase (type IV) activity with an IC₅₀ of 10.4±0.4 μM. In contrast, phosphodiesterase I, III and V activities were inhibited by Butein above 100 μM^[1].
Butein, a plant polyphenol, is a specific protein tyrosine kinase inhibitor. Butein inhibits not only the EGF-stimulated auto-phosphotyrosine level of EGFR in HepG2 cells but also tyrosine-specific protein kinase activities of EGFR (IC₅₀=16 μM) and p60^c-src (IC₅₀=65 μM) in vitro^[2].
Butein (10, 20, and 40 μM; 24, 48, and 72 hours) inhibits cell growth in a dose- and time-dependent manner^[3].
Butein exhibits anticancer activity through the inhibition of the activation of PKB/AKT and MAPK pathways, which are two pathways known to be involved in resistance to cisplatin. Butein (20 μM) decreases phosphorylation of AKT, ERK and p38 following 24 h of co-treatment with Cisplatin (20 μM)^[3].

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

Cell Viability Assay^[3]

Cell Line:

HeLa cells
Concentration:

10, 20, and 40 μM
Incubation Time:

24, 48, and 72 hours
Result:

Inhibited cell growth in a dose- and time-dependent manner.

Western Blot Analysis^[3]

Cell Line:

HeLa cells
Concentration:

20 µM
Incubation Time:

24 hours
Result:

Decreased phosphorylation of AKT, ERK and p38 co-treatment with Cisplatin (20 µM).

In Vivo

Butein (2 mg/kg every 2 days) in combination with Cisplatin (2 mg/kg every 2 days) for 3 weeks suppresses tumor growth in vivo^[3].

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

Animal Model:

Nude mice (12 female 6- or 7-week old) with subcutaneous tumor xenografts^[3]
Dosage:

2 mg/kg
Administration:

Intraperitoneally; every 2 days; for 3 weeks
Result:

Enhanced the antitumor effects of Cisplatin in vivo.

Chemical Information

CAS No. 487-52-5
Appearance Solid
Molecular Weight 272.25
Formula C₁₅H₁₂O₅
Color Light yellow to brown
SMILES

OC1=CC=C(C(/C=C/C2=CC(O)=C(O)C=C2)=O)C(O)=C1
Synonyms

2’,3,4,4’-tetrahydroxy Chalcone
Structure Classification
- Flavonoids
- Chalcones
- Phenols
- Polyphenols
Initial Source
- Plants
- other families
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (6)

All Cell Proliferation/Viability AssayWBCell Imaging/StainingELISAIn Vivo Efficacy Study

Sort by:

Journal Impact Factor

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
Cell Commun Signal

Homotherapy for heteropathy: therapeutic effect of Butein in NLRP3-driven diseases. [Abstract]

2024 Jun 7;22(1):315. PMID: 38849890

Butein purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2024 Jun 7;22(1):315. [Abstract]

Cell viability of Butein (10, 20, 30, 40, 50, 60, 70, 80, 90 μM).

Butein purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2024 Jun 7;22(1):315. [Abstract]

BMDMs were primed with LPS for 4 h and then treated with Butein (2.5, 5, 10 μM) for 1 h before stimulation with Nigericin for 1 h. Western blot analyses of pro-IL-1β, caspase-1 p45, NLRP3, and ASC in lysates (Input) and IL-1β p17, caspase-1 p20 in culture supernatants (SN).

Butein purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2024 Jun 7;22(1):315. [Abstract]

LPS-primed BMDMs were treated with Butein (2.5, 5, 10 μM) for 1 h prior to stimulation with Nigericin for 1 h. BMDMs were then stained with Hoechst 33,342 followed by PI. Cells were observed by fluorescence microscope.

Butein purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2024 Jun 7;22(1):315. [Abstract]

BMDMs were treated with LPS for 4 h and then stimulated with Butein (2.5, 5, 10 μM) for 1 h (butein after LPS) or treated with butein for 1 h and then stimulated with LPS for 4 h (butein before LPS). TNF-α and IL-6 secretion in SN was measured by ELISA.

Butein purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2024 Jun 7;22(1):315. [Abstract]

Mice received Butein (10, or 20 mg/kg) by intragastric gavage during the modeling period. Representative the colon lengths.
ACS Omega

Identification of Phialomustin‑B (PHL-B) as a Novel Natural TRPA1 Channel Inhibitor. [Abstract]

2025 Aug 21;10(34):39192-39202. PMID: 40918390
J Mol Histol

Butein attenuates cardiac fibrosis by mediating TGF-β1/Smad signaling pathway after myocardial infarction. [Abstract]

2025 Oct 22;56(6):352. PMID: 41123714
J Gene Med

Exploring the mechanism underlying the therapeutic effects of butein in colorectal cancer using network pharmacology and single-cell RNA sequencing data. [Abstract]

2024 Jan;26(1):e3628. PMID: 37963584
Oxid Med Cell Longev

The Sirt1/P53 Axis in Diabetic Intervertebral Disc Degeneration Pathogenesis and Therapeutics. [Abstract]

2019 Sep 9;2019:7959573. PMID: 31583043

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (183.65 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

3.6731 mL

18.3655 mL

36.7309 mL

5 mM

0.7346 mL

3.6731 mL

7.3462 mL

10 mM

0.3673 mL

1.8365 mL

3.6731 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (9.18 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: 1.67 mg/mL (6.13 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 1.67 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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)
Handling Instructions (2659 KB)

References

[1]. Yu SM, et al. Endothelium-dependent relaxation of rat aorta by butein, a novel cyclic AMP-specific phosphodiesterase inhibitor.Eur J Pharmacol. 1995 Jun 23;280(1):69-77. [Content Brief]

[2]. Yang EB, et al. Butein, a specific protein tyrosine kinase inhibitor.Biochem Biophys Res Commun. 1998 Apr 17;245(2):435-8. [Content Brief]

[3]. Zhang L, et al. Butein sensitizes HeLa cells to cisplatin through the AKT and ERK/p38 MAPK pathways by targeting FoxO3a.Int J Mol Med. 2015 Oct;36(4):957-66. [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, 6 months; -20°C, 1 month. 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	3.6731 mL	18.3655 mL	36.7309 mL	91.8274 mL
	5 mM	0.7346 mL	3.6731 mL	7.3462 mL	18.3655 mL
	10 mM	0.3673 mL	1.8365 mL	3.6731 mL	9.1827 mL
	15 mM	0.2449 mL	1.2244 mL	2.4487 mL	6.1218 mL
	20 mM	0.1837 mL	0.9183 mL	1.8365 mL	4.5914 mL
	25 mM	0.1469 mL	0.7346 mL	1.4692 mL	3.6731 mL
	30 mM	0.1224 mL	0.6122 mL	1.2244 mL	3.0609 mL
	40 mM	0.0918 mL	0.4591 mL	0.9183 mL	2.2957 mL
	50 mM	0.0735 mL	0.3673 mL	0.7346 mL	1.8365 mL
	60 mM	0.0612 mL	0.3061 mL	0.6122 mL	1.5305 mL
	80 mM	0.0459 mL	0.2296 mL	0.4591 mL	1.1478 mL
	100 mM	0.0367 mL	0.1837 mL	0.3673 mL	0.9183 mL

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Product Name:
CAS No.:
Species:
Purity:
Quantity:

Butein

Apoptosis Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Metabolism/Protease Compound Library

Protein Tyrosine Kinase Compound Library

Natural Product Library

Anti-Cancer Compound Library

Autophagy Compound Library

Differentiation Inducing Compound Library

Lipid Compound Library

Medicine Food Homology Compound Library

Phenols Library

Traditional Chinese Medicine Active Compound Library

Flavonoids Library

Anti-Alzheimer's Disease Compound Library

Anti-Hepatitis C Virus Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Neurodegenerative Disease-related Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Food-Sourced Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Cancer Natural Product Library

Antidepressant Compound Library

Anti-inflammatory Traditional Chinese Medicine Active Compound Library

Plant-Sourced Natural Product Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Anti-Aging Natural Product Library

Cancer Stem Cells Compound Library

Metabolic Enzyme Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Mitochondrial Toxicity Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cytokine Inhibitors Library

Cell Death Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Natural Product Library Plus

Natural Product and Natural Product-Like Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Miao Ethnicity Medicine Compound Library

PBCRBS Traditional Chinese Medicine Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

RO5 Drug-like Natural Product Library

Cell Proliferation Compound Library

Flavor Compound Library

High-Throughput Bioactive Compound Library

High-Throughput Natural Product Library

Ancient Chinese Classical Formulas Traditional Chinese Medicine Active Compound Library

Antitussive and Antiasthmatic Traditional Chinese Medicine Active Compound Library

Diarrhea-Related Traditional Chinese Medicine Active Compound Library

Posttranslational Modification Library

Mongolian Medicine Compound Library

Mass Spectrometry Natural Product Library

Publications Citing Use of MedChemExpress (MCE) Butein

All EGFR Isoforms

All Phosphodiesterase (PDE) Isoforms

Biological Activity

Chemical Information

Publications (6)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Butein Related Classifications

Cat. No.: HY-16558