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  3. Butein

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

製品番号: HY-16558 純度: 99.95%
COA 取扱説明書 Technical Support

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).

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Butein 構造式

Butein 構造式

CAS 番号 : 487-52-5

容量 価格(税別) 在庫状況 数量
無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 99 在庫あり
Solution
10 mM * 1 mL in DMSO USD 99 在庫あり
Solid
2 mg USD 66 在庫あり
5 mg USD 106 在庫あり
10 mg USD 158 在庫あり
50 mg USD 440 在庫あり
100 mg USD 700 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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カスタマーレビュー

Based on 4 publication(s) in Google Scholar

Other Forms of Butein:

Top Publications Citing Use of Products

EGFR アイソフォーム固有の製品をすべて表示:

Phosphodiesterase (PDE) アイソフォーム固有の製品をすべて表示:

  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

  • カスタマーレビュー

製品説明

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)

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
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]
体外実験

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.

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).
体内実験

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.
分子量

272.25

Synonyms

2’,3,4,4’-tetrahydroxy Chalcone

分子式

C15H12O5

CAS 番号
Appearance

Solid

Color

Light yellow to brown

SMILES

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

Structure Classification
Initial Source
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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
10 mM 0.3673 mL 1.8365 mL 3.6731 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
×
Volume
×
Molecular Weight *

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

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始)

C1

×
体積 (開始)

V1

=
濃度 (終了)

C2

×
体積 (終了)

V2

体内:

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.
純度とドキュメンテーション

純度: 99.95%

参考文献

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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  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
× = ×
C1   V1   C2   V2
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.

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製品名:
Butein
製品番号:
HY-16558
数量:
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