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

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

Cat. No.: HY-16558 Purity: 99.95%
Handling Instructions

Butein, isolated from Dalbergia odorifera T. Chen, 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

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 90 In-stock
Estimated Time of Arrival: December 31
2 mg USD 60 In-stock
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5 mg USD 96 In-stock
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10 mg USD 144 In-stock
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50 mg USD 540 In-stock
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100 mg USD 900 In-stock
Estimated Time of Arrival: December 31
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Based on 2 publication(s) in Google Scholar

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Description

Butein, isolated from Dalbergia odorifera T. Chen, 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].

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].

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.

487-52-5

SMILES

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

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 : ≥ 35 mg/mL (128.56 mM)

*"≥" means soluble, but saturation unknown.

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
10 mM 0.3673 mL 1.8365 mL 3.6731 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

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

  • 2.

    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

*All of the co-solvents are provided by MCE.
References
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Keywords:

Butein2’,3,4,4’-tetrahydroxy ChalconeEGFRAutophagyApoptosisPhosphodiesterase (PDE)Epidermal growth factor receptorErbB-1HER1PKBAKTMAPKp38ERKFoxO3aHeLaHepG2cellSIRT1PDE4Inhibitorinhibitorinhibit

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