2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor Cell Cycle/DNA Damage
  3. RAR/RXR PPAR Aldose Reductase
  4. Drupanin

Drupanin is an orally active and selective AKR1C3 enzyme inhibitor and an RXRα agonist with an EC50 value of 4.8 μM, which is found in green propolis. Drupanin also activates PPARγ moderately. Drupanin induces adipogenesis and elevates aP2 mRNA levels in 3T3-L1 fibroblasts Drupanin has the potential for the research of breast and prostate cancers.

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Drupanin

Drupanin 構造式

CAS 番号 : 53755-58-1

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 330 在庫あり
Solution
10 mM * 1 mL in DMSO USD 330 在庫あり
Solid
5 mg $300 在庫あり
10 mg $480 在庫あり
25 mg $960 在庫あり
50 mg $1550 在庫あり
100 mg $2500 在庫あり
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500 mg   お問い合わせ  

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Drupanin 関連抗体

Top Publications Citing Use of Products

RAR/RXR アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
RXRα RXRβ RXRγ

PPAR アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
PPARα PPARβ/δ PPARγ PPAR PPARδ

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製品説明

Drupanin is an orally active and selective AKR1C3 enzyme inhibitor and an RXRα agonist with an EC50 value of 4.8 μM, which is found in green propolis. Drupanin also activates PPARγ moderately. Drupanin induces adipogenesis and elevates aP2 mRNA levels in 3T3-L1 fibroblasts Drupanin has the potential for the research of breast and prostate cancers[1][2][3].

IC50 & Target

PPARα

39.0 μM (EC50)

PPARγ

14.6 μM (EC50)

PPARδ

N.D.(not d ()

RXR α

2.1 μM (EC50)

RXRγ

4.6 μM (EC50)

Cellular Effect
Cell Line Type Value Description References
DU-145 IC50
> 200 μM
Compound: 2
Antiproliferative activity against human DU-145 cells assessed as cell viability for 72 hrs by MTT assay
Antiproliferative activity against human DU-145 cells assessed as cell viability for 72 hrs by MTT assay
[PMID: 34454129]
HEK293 IC50
25.6 μM
Compound: 9
Modulation of HIF1 expressed in HEK293 cells assessed as luciferase activity under hypoxic condition after 24 hrs by luminometer analysis
Modulation of HIF1 expressed in HEK293 cells assessed as luciferase activity under hypoxic condition after 24 hrs by luminometer analysis
[PMID: 21865046]
HeLa IC50
10.3 μg/mL
Compound: 3
Antiallergic activity in Ca(2+)-stimulated differentiated human HeLa cells assessed as inhibition of cys-leukotriene release after 6 days by ELISA
Antiallergic activity in Ca(2+)-stimulated differentiated human HeLa cells assessed as inhibition of cys-leukotriene release after 6 days by ELISA
[PMID: 19942440]
MCF-10A CC50
> 200 μM
Compound: 2
Cytotoxicity against human MCF-10A cells assessed as cell viability for 72 hrs by MTT assay
Cytotoxicity against human MCF-10A cells assessed as cell viability for 72 hrs by MTT assay
[PMID: 34454129]
MCF7 IC50
> 200 μM
Compound: 2
Antiproliferative activity against human MCF7 cells assessed as cell viability for 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as cell viability for 72 hrs by MTT assay
[PMID: 34454129]
MDA-MB-231 IC50
> 200 μM
Compound: 2
Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability for 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability for 72 hrs by MTT assay
[PMID: 34454129]
PC-3 IC50
> 200 μM
Compound: 2
Antiproliferative activity against human PC-3 cells assessed as cell viability for 72 hrs by MTT assay
Antiproliferative activity against human PC-3 cells assessed as cell viability for 72 hrs by MTT assay
[PMID: 34454129]
PNT2 CC50
> 200 μM
Compound: 2
Cytotoxicity against human PNT2 cells assessed as cell viability for 72 hrs by MTT assay
Cytotoxicity against human PNT2 cells assessed as cell viability for 72 hrs by MTT assay
[PMID: 34454129]
体外実験

Drupanin (2.5-25 μM, 1 h) stimulates the interaction between PPARγ and cAMP responsive element-binding protein-binding protein in HEK 293 cells (EC50 value: 14.6 μM)[2].
Drupanin (25 μM, 5 days) enhances the adipogenesis of mouse 3T3-L1 fibroblasts[2].
Drupanin (101.7-103.5 μM, 48 h) shows cytotoxic effects on PC3 and LnCaP cells[3].

The EC50 values of Drupanin for each RXR subtype cofactor[2]

subtypes RXRα RXRγ RXRδ
EC50 (μM) 2.1 4.6 7.0

The EC50 values of Drupanin for each PPAR subtype cofactor[2]
subtypes PPARα PPARγ PPARδ
EC50 (μM) 39.0 14.6 N.D. (not detected)

Growth Inhibitory Effect of Drupanin[3]
NCI-H460 MCF7 PC3 LnCaP HL60 U937 S-180
GI50 (μM) 158.5 141.3 501.2 338.8 166.0 323.6 416.9
LC50 (μM) N.D. N.D. 885.1 1331.4 N.D. N.D. N.D.

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

Drupanin 関連抗体

Real Time qPCR[2]

Cell Line: HEK 293 cells
Concentration: 2.5-25 μM
Incubation Time: 1 h
Result: Slightly increased luciferase activity for each PPAR subtype (α, γ, and δ).
体内実験

Drupanin (100 mg/kg, p.o., daily for 28 days) inhibits the tumor growth and induces genotoxic damage in DDY mice allografted with sarcoma S-180[3].

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

Animal Model: DDY mice allografted with sarcoma S-180[2]
Dosage: 100 mg/kg
Administration: p.o., daily for 28 days
Result: Resulted in a significant decrease of tumor mass at a dosage of 100 mg/kg/d (p<0.05) and caused DNA damage in sarcoma S-180.
分子量

232.28

分子式

C14H16O3
CAS 番号
Appearance

Solid

Color

Off-white to light yellow

SMILES

C/C(C)=C\CC1=C(C=CC(/C=C/C(O)=O)=C1)O
Structure Classification
Initial Source

A. Mellifera
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 : 100 mg/mL (430.51 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 4.3051 mL 21.5257 mL 43.0515 mL
5 mM 0.8610 mL 4.3051 mL 8.6103 mL
10 mM 0.4305 mL 2.1526 mL 4.3051 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)

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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）

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In Vivo Dissolution Calculator
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Calculation results:
Working solution concentration: mg/mL
純度とドキュメンテーション
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 4.3051 mL 21.5257 mL 43.0515 mL 107.6287 mL
5 mM 0.8610 mL 4.3051 mL 8.6103 mL 21.5257 mL
10 mM 0.4305 mL 2.1526 mL 4.3051 mL 10.7629 mL
15 mM 0.2870 mL 1.4350 mL 2.8701 mL 7.1752 mL
20 mM 0.2153 mL 1.0763 mL 2.1526 mL 5.3814 mL
25 mM 0.1722 mL 0.8610 mL 1.7221 mL 4.3051 mL
30 mM 0.1435 mL 0.7175 mL 1.4350 mL 3.5876 mL
40 mM 0.1076 mL 0.5381 mL 1.0763 mL 2.6907 mL
50 mM 0.0861 mL 0.4305 mL 0.8610 mL 2.1526 mL
60 mM 0.0718 mL 0.3588 mL 0.7175 mL 1.7938 mL
80 mM 0.0538 mL 0.2691 mL 0.5381 mL 1.3454 mL
100 mM 0.0431 mL 0.2153 mL 0.4305 mL 1.0763 mL
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Drupanin Related Classifications

  • 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.

Keywords:

Drupanin53755-58-1RAR/RXRPPARAldose ReductaseRetinoic acid receptorsRetinoid X receptorsPeroxisome proliferator-activated receptorsorally activeAKR1C3 enzymeRXRαPPARγ3T3-L1 fibroblastsbreast and prostate cancersInhibitorinhibitorinhibit

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製品名:
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製品番号:
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