2. Metabolic Enzyme/Protease
  3. Cytochrome P450
  4. Dafadine-A

Dafadine-A is a selective inhibitor of DAF-9 cytochrome P450 in the nematode Caenorhabditis elegans. Dafadine-A inhibits the mammalian ortholog of DAF-9 (CYP27A1). Dafadine-A does not inhibits DAF-12 and sterol- and oxysterol-metabolizing P450s.

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Dafadine-A Chemical Structure

Dafadine-A Chemical Structure

CAS No. : 1065506-69-5

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Based on 1 publication(s) in Google Scholar

Dafadine-A Related Antibodies

Top Publications Citing Use of Products

View All Cytochrome P450 Isoform Specific Products:

View All Isoforms
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Dafadine-A is a selective inhibitor of DAF-9 cytochrome P450 in the nematode Caenorhabditis elegans. Dafadine-A inhibits the mammalian ortholog of DAF-9 (CYP27A1). Dafadine-A does not inhibits DAF-12 and sterol- and oxysterol-metabolizing P450s[1].

In Vitro

Dafadine-A (12.5 μM; treating wild-type Caenorhabditis elegans) induces a constitutive dauer formation (Daf-c) phenotype in more than 30% of worms[1].
Dafadine-A (25 μM; treating wild-type Caenorhabditis elegans) causes a protruding vulva (Pvl) phenotype and distal-tip cell migration (Mig) defects in over 60% of worms[1].
Dafadine-A (5 μM) inhibits the ability of CYP27A1 to metabolize 4-cholesten-3-one[1].
Dafadine-A extends the lifespan of wild-type Caenorhabditis elegans by 29%[1].
Dafadine-A (5-10 μM; 48 h) dramatically inhibits cholesterol-induced melanoma spheroid propagation and downregulates Rap1A/Rap1B expression and phosphorylated AKT1-thr308/309[2].
Dafadine-A (10 μM; 48 h) significantly enhances Vemurafenib (HY-12057)-induced apoptosis[2].

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

Dafadine-A Related Antibodies

Apoptosis Analysis[2]

Cell Line: A375 and A2058 melanoma cells
Concentration: 10 μM
Incubation Time: 48 h
Result: Significantly enhanced Vemurafenib-induced apoptosis.

Western Blot Analysis[2]

Cell Line: A375 and A2058 melanoma cells
Concentration: 5 μM, 10 μM
Incubation Time: 48 h
Result: Inhibited cholesterol-induced melanoma spheroid propagation, downregulated Rap1A/Rap1B expression and phosphorylated AKT1-thr308/309.
Molecular Weight

391.46

Formula

C23H25N3O3
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(N1CCC(C2=CC=NC=C2)CC1)C3=NOC(COC4=C(C)C=CC=C4C)=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (127.73 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 2.5545 mL 12.7727 mL 25.5454 mL
5 mM 0.5109 mL 2.5545 mL 5.1091 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

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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)

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Volume (start)

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C2

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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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.39 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 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.39 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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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, PEG300/PEG400, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 98.94%

Data Sheet (274 KB) SDS (251 KB)

COA (248 KB)LCMS (111 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5545 mL 12.7727 mL 25.5454 mL 63.8635 mL
5 mM 0.5109 mL 2.5545 mL 5.1091 mL 12.7727 mL
10 mM 0.2555 mL 1.2773 mL 2.5545 mL 6.3863 mL
15 mM 0.1703 mL 0.8515 mL 1.7030 mL 4.2576 mL
20 mM 0.1277 mL 0.6386 mL 1.2773 mL 3.1932 mL
25 mM 0.1022 mL 0.5109 mL 1.0218 mL 2.5545 mL
30 mM 0.0852 mL 0.4258 mL 0.8515 mL 2.1288 mL
40 mM 0.0639 mL 0.3193 mL 0.6386 mL 1.5966 mL
50 mM 0.0511 mL 0.2555 mL 0.5109 mL 1.2773 mL
60 mM 0.0426 mL 0.2129 mL 0.4258 mL 1.0644 mL
80 mM 0.0319 mL 0.1597 mL 0.3193 mL 0.7983 mL
100 mM 0.0255 mL 0.1277 mL 0.2555 mL 0.6386 mL
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Dafadine-A Related Classifications

Keywords:

Dafadine-A1065506-69-5Cytochrome P450CYPsAKT1-thr308/309 Rap1A/Rap1BDAF-9Caenorhabditis elegansInhibitorinhibitorinhibit

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