2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Autophagy Apoptosis Metabolic Enzyme/Protease
  3. EGFR Autophagy Apoptosis Phosphodiesterase (PDE)
  4. Butein

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

Cat. No.: HY-16558 Purity: 99.95%
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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 p60c-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.

Butein Chemical Structure

Butein Chemical Structure

CAS No. : 487-52-5

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Based on 4 publication(s) in Google Scholar

Other Forms of Butein:

Butein Related Antibodies

Top Publications Citing Use of Products

View All EGFR Isoform Specific Products:

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

View All Phosphodiesterase (PDE) Isoform Specific Products:

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PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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 p60c-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)

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 p60c-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.

Butein Related Antibodies

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.
Molecular Weight

272.25

Formula

C15H12O5
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

OC1=CC=C(C(/C=C/C2=CC(O)=C(O)C=C2)=O)C(O)=C1
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 6 months
-20°C 1 month
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.6731 mL 18.3655 mL 36.7309 mL
5 mM 0.7346 mL 3.6731 mL 7.3462 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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% (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.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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: 99.95%

COA (247 KB) HNMR (270 KB) RP-HPLC (275 KB)

Handling Instructions (2659 KB)
References

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. 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
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Butein 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.

Keywords:

Butein487-52-52’,3,4,4’-tetrahydroxy ChalconeEGFRAutophagyApoptosisPhosphodiesterase (PDE)Epidermal growth factor receptorErbB-1HER1PKBAKTMAPKp38ERKFoxO3aHeLaHepG2cellSIRT1PDE4Inhibitorinhibitorinhibit

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