2. Neuronal Signaling Metabolic Enzyme/Protease Apoptosis
  3. Monoamine Oxidase Dopamine β-hydroxylase Apoptosis
  4. 4-Hydroxyderricin

4-Hydroxyderricin, the major active ingredients of Angelica keiskei Koidzumi, is an orally active, potent selective MAO-B (Monoamine oxidase inhibitors) inhibitor with an IC50 of 3.43 μM. 4-Hydroxyderricin also mildly inhibits dopamine β (DBH)-hydroxylase activity. 4-Hydroxyderricin has antidepressant activity, anti-allergic, anti-diabetic, anti-oxidant, and antitumor effects. 4-Hydroxyderricin promotes apoptosis and cell cycle arrest through regulating PI3K/AKT/mTOR pathway in hepatocellular cells. 4-Hydroxyderricin inhibits osteoclast formation and accelerates osteoblast differentiation. 4-Hydroxyderricin is promising for research of inflammatory diseases.

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4-Hydroxyderricin Chemical Structure

4-Hydroxyderricin Chemical Structure

CAS No. : 55912-03-3

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Based on 1 publication(s) in Google Scholar

4-Hydroxyderricin Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE 4-Hydroxyderricin

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Description

4-Hydroxyderricin, the major active ingredients of Angelica keiskei Koidzumi, is an orally active, potent selective MAO-B (Monoamine oxidase inhibitors) inhibitor with an IC50 of 3.43 μM. 4-Hydroxyderricin also mildly inhibits dopamine β (DBH)-hydroxylase activity. 4-Hydroxyderricin has antidepressant activity, anti-allergic, anti-diabetic, anti-oxidant, and antitumor effects. 4-Hydroxyderricin promotes apoptosis and cell cycle arrest through regulating PI3K/AKT/mTOR pathway in hepatocellular cells. 4-Hydroxyderricin inhibits osteoclast formation and accelerates osteoblast differentiation[1]. 4-Hydroxyderricin is promising for research of inflammatory diseases[1][2][3][4][5].

IC50 & Target

IC50: 3.43 μM (MAO-B)[1]
In Vitro

4-Hydroxyderricin (0-10 μM, 48 h, 2, 7, 9 or 11 days) completely inhibits the formation of multinucleated osteoclastic cells, dose-dependently decreases RANKL mRNA expression in ST2 cells, increases the activity of alkaline phosphatase and the deposition of calcium in MC3T3-E1 cells and decreases H2O2 levels in osteoblasts[2].
4-Hydroxyderricin (1-10 μM, 24 h) and Xanthoangelol (1-10 μM, 24 h) down-regulates LPS (HY-D1056)-mediated production of NO and TNF-α , reduces the DNA-binding activity of AP-1 and inhibis the phosphorylation of NF-κB in mouse macrophages[4].
4-Hydroxyderricin (0-100 μM, 24 h and 48 h) inhibits the proliferation and metastasis, induces apoptosis by activating the mitochondrial apoptosis pathway and cell cycle arrest in HepG2 and Huh7 cells[5].

The IC50 values (micro mole) of 4-Hydroxyderricin from A. keiskei against MAO-A, MAO-B and DBH activities[1]

Compounds MAO-A MAO-B DBH
4-hydroxyderricin 3520 3.43 12.0

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

4-Hydroxyderricin Related Antibodies

Real Time qPCR[3]

Cell Line: ST2 cells
Concentration: 0-10 μM
Incubation Time: 2 days
Result: Dose-dependently decreased RANKL mRNA expression in ST2 cells.

Cell Viability Assay[5]

Cell Line: HepG2 and Huh7 cells
Concentration: 0-100 μM
Incubation Time: 24 h and 48 h
Result: Decreased the HepG2 and Huh7 cell viability with a concentration higher than 20 µM.

Cell Migration Assay [3]

Cell Line: HepG2 and Huh7 cells
Concentration: 20 and 40 μM
Incubation Time: 48 h
Result: Effectively inhibit the migration process of HepG2 and Huh7 cells.
In Vivo

4-Hydroxyderricin (25 or 50 mg/kg, p.o., twice daily for 14 days) inhibits tumor growth, prolongs the survival time and increases the survival rate in mice with subcutaneously implanted Lewis lung carcinoma (LLC)[3].

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

Animal Model: Mice with subcutaneously implanted LLC[3]
Dosage: 25 or 50 mg/kg
Administration: p.o., twice daily for 14 days
Result: Significantly inhibited tumor growth on days 8 to 14, prolonged the survival time and increased the survival rate in mice with subcutaneously implanted LLC, inhibited metastasis to the lung in tumor-removed mice.
Molecular Weight

338.40

Formula

C21H22O4
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=CC=C(OC)C(C/C=C(C)\C)=C1O)/C=C/C2=CC=C(O)C=C2
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (295.51 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 2.9551 mL 14.7754 mL 29.5508 mL
5 mM 0.5910 mL 2.9551 mL 5.9102 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 (protect from light). 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
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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 (7.39 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.
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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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.
Purity & Documentation

Purity: 99.97%

COA (245 KB) HNMR (216 KB) CNMR (237 KB) RP-HPLC (208 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, 6 months; -20°C, 1 month (protect from light). 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 2.9551 mL 14.7754 mL 29.5508 mL 73.8771 mL
5 mM 0.5910 mL 2.9551 mL 5.9102 mL 14.7754 mL
10 mM 0.2955 mL 1.4775 mL 2.9551 mL 7.3877 mL
15 mM 0.1970 mL 0.9850 mL 1.9701 mL 4.9251 mL
20 mM 0.1478 mL 0.7388 mL 1.4775 mL 3.6939 mL
25 mM 0.1182 mL 0.5910 mL 1.1820 mL 2.9551 mL
30 mM 0.0985 mL 0.4925 mL 0.9850 mL 2.4626 mL
40 mM 0.0739 mL 0.3694 mL 0.7388 mL 1.8469 mL
50 mM 0.0591 mL 0.2955 mL 0.5910 mL 1.4775 mL
60 mM 0.0493 mL 0.2463 mL 0.4925 mL 1.2313 mL
80 mM 0.0369 mL 0.1847 mL 0.3694 mL 0.9235 mL
100 mM 0.0296 mL 0.1478 mL 0.2955 mL 0.7388 mL
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4-Hydroxyderricin 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:

4-Hydroxyderricin55912-03-3Monoamine OxidaseDopamine β-hydroxylaseApoptosisMAODopamine beta-hydroxylaseDopamine beta-monooxygenaseDopamine β-monooxygenaseorally activeMAO-BDBHantidepressant activityanti-allergicanti-diabeticantioxidantantitumor effectsinflammatory diseasesInhibitorinhibitorinhibit

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