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

Drupanin is an orally active selective AKR1C3 enzyme inhibitor and an RXRα agonist with an EC50 value of 4.8 μM, which is isolated from 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.

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

Drupanin Chemical Structure

Drupanin Chemical Structure

CAS No. : 53755-58-1

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

Drupanin Related Antibodies

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PPARα PPARβ/δ PPARγ PPAR PPARδ

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Description

Drupanin is an orally active selective AKR1C3 enzyme inhibitor and an RXRα agonist with an EC50 value of 4.8 μM, which is isolated from 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].

In Vitro

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 (μM) HL60 U937 S-180
GI50 158.5 141.3 501.2 338.8 166.0 323.6 416.9
LC50 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 Related Antibodies

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).
In Vivo

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.
Molecular Weight

232.28

Formula

C14H16O3
CAS No.
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
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 : 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
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.

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation
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 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

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/RXRPPARRetinoic acid receptorsRetinoid X receptorsPeroxisome proliferator-activated receptorsorally activeAKR1C3 enzymeRXRαPPARγ3T3-L1 fibroblastsbreast and prostate cancersInhibitorinhibitorinhibit

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