2. Neuronal Signaling Protein Tyrosine Kinase/RTK JAK/STAT Signaling Epigenetics Stem Cell/Wnt NF-κB Immunology/Inflammation Metabolic Enzyme/Protease
  3. Monoamine Oxidase JAK IKK STAT NO Synthase Cytochrome P450
  4. Desmethoxyyangonin

Desmethoxyyangonin  (Synonyms: Demethoxyyangonin; 5,6-Dehydrokavain)

Cat. No.: HY-N0918 Purity: 99.46%
SDS
COA
Handling Instructions Technical Support

Desmethoxyyangonin is one of the six major kavalactones found in the Piper methysticum (kava) plant. Desmethoxyyangonin is a selective inhibitor of monoamine oxidase-B (MAO-B) (IC50: 0.123  µM). Desmethoxyyangonin exerts anti-inflammatory effects by inhibiting Jak2/STAT3 and IKK signaling pathways. Desmethoxyyangonin induces CYP3A23 expression and leads to skeletal muscle relaxation.

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Desmethoxyyangonin Chemical Structure

Desmethoxyyangonin Chemical Structure

CAS No. : 15345-89-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

Other Forms of Desmethoxyyangonin:

Desmethoxyyangonin Related Antibodies

Top Publications Citing Use of Products

View All Monoamine Oxidase Isoform Specific Products:

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MAO-A MAO-B

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JAK1 JAK2 JAK3 Tyk2 JAK

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IKK-α IKK-β IKK IKKε TBK1

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STAT3 STAT5 STAT6 STAT1

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nNOS iNOS eNOS

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

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Desmethoxyyangonin is one of the six major kavalactones found in the Piper methysticum (kava) plant. Desmethoxyyangonin is a selective inhibitor of monoamine oxidase-B (MAO-B) (IC50: 0.123  µM). Desmethoxyyangonin exerts anti-inflammatory effects by inhibiting Jak2/STAT3 and IKK signaling pathways. Desmethoxyyangonin induces CYP3A23 expression and leads to skeletal muscle relaxation[1][2][3][4].

IC50 & Target[1][2][3][4]

MAO-B

0.123 μM (IC50)

MAO-A

1.850 μM (IC50)

JAK2

 

STAT3

 

iNOS

 

Cellular Effect
Cell Line Type Value Description References
A549 IC50
33 μg/mL
Compound: Desmethoxyyangonin
Inhibition of TNF-alpha-induced NF-kappaB expressed in human A549 cells treated 1 hr after TNFalpha challenge measured after 6 hrs by luciferase reporter gene assay
Inhibition of TNF-alpha-induced NF-kappaB expressed in human A549 cells treated 1 hr after TNFalpha challenge measured after 6 hrs by luciferase reporter gene assay
[PMID: 19716299]
HT-1080 ED50
> 100 μM
Compound: 13
Antiproliferative activity against human HT1080 cells by MTT assay
Antiproliferative activity against human HT1080 cells by MTT assay
[PMID: 11277741]
L6 IC50
160 μM
Compound: 4
Cytotoxicity against rat L6 myoblasts after 72 hrs by alamar blue assay
Cytotoxicity against rat L6 myoblasts after 72 hrs by alamar blue assay
[PMID: 22285027]
In Vitro

Desmethoxyyangonin (10-200 µM, 7-19 h) inhibits the activity of pro-inflammatory mediators in LPS-induced macrophages RAW 264.7[2].
Desmethoxyyangonin (50 µM, 3-9 h) inhibits Jak2/STAT3 and IKK signaling pathways in LPS-induced macrophages RAW 264.7[2].
Desmethoxyyangonin (25-100 µM, 48 h) inhibits CD4 cell activation and proliferation in a dose-dependent manner[2].
Desmethoxyyangonin (2-100 µM, 24-72 h) induces the expression of CYP3A23[4].

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

Desmethoxyyangonin Related Antibodies

Western Blot Analysis[2]

Cell Line: RAW 264.7 cells incubated with 100 ng/mL LPS
Concentration: 10, 25, 50 ,75, 100, 150, 200 µM
Incubation Time: 19; 3, 5, 9 h
Result: Down-regulated iNOS protein levels.
Down-regulated p- Jak2, STAT3, p- STAT3, IKK, IKBα protein levels.

ELISA Assay[2]

Cell Line: RAW 264.7 cells incubated with 100 ng/mL LPS
Concentration: 10, 25, 50 ,75, 100 µM
Incubation Time: 18 h
Result: Down-regulated TNF-α and IL-6 concentrations.
In Vivo

Desmethoxyyangonin (1 and 10 mg/kg, i.p., 3 days) reduces liver damage in the mouse LPS/D-GalN-induced fulminant hepatitis model[2].
Desmethoxyyangonin (20 mg/kg, i.p.) induces skeletal muscle relaxation in male Wistar rats[3].

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

Animal Model: Mice LPS/D-GalN-induced fulminant hepatitis model (ICR mice, 4 weeks old; 1 h before injection with 500 ng LPS and 25 mg D-GalN in 250 μL saline)[2]
Dosage: 1 and 10 mg/kg
Administration: Intraperitoneal injection (i.p.), 3 days
Result: Inhibited AST and ALT activity (1.7-2.4 times).
Reduced apoptotic cells in liver tissue.
Increased the survival rate (90%).
Molecular Weight

228.24

Formula

C14H12O3
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C1C=C(OC)C=C(/C=C/C2=CC=CC=C2)O1
Structure Classification
Initial Source
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 : 25 mg/mL (109.53 mM; ultrasonic and warming and heat to 60°C; 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 4.3814 mL 21.9068 mL 43.8135 mL
5 mM 0.8763 mL 4.3814 mL 8.7627 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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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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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    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (10.95 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

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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:
%
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% 
+
%
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%
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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.
Purity & Documentation

Purity: 99.46%

SDS (393 KB)

COA (246 KB) HNMR (246 KB) LCMS (94 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. 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 4.3814 mL 21.9068 mL 43.8135 mL 109.5338 mL
5 mM 0.8763 mL 4.3814 mL 8.7627 mL 21.9068 mL
10 mM 0.4381 mL 2.1907 mL 4.3814 mL 10.9534 mL
15 mM 0.2921 mL 1.4605 mL 2.9209 mL 7.3023 mL
20 mM 0.2191 mL 1.0953 mL 2.1907 mL 5.4767 mL
25 mM 0.1753 mL 0.8763 mL 1.7525 mL 4.3814 mL
30 mM 0.1460 mL 0.7302 mL 1.4605 mL 3.6511 mL
40 mM 0.1095 mL 0.5477 mL 1.0953 mL 2.7383 mL
50 mM 0.0876 mL 0.4381 mL 0.8763 mL 2.1907 mL
60 mM 0.0730 mL 0.3651 mL 0.7302 mL 1.8256 mL
80 mM 0.0548 mL 0.2738 mL 0.5477 mL 1.3692 mL
100 mM 0.0438 mL 0.2191 mL 0.4381 mL 1.0953 mL
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Desmethoxyyangonin 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:

Desmethoxyyangonin15345-89-8Demethoxyyangonin 5,6-DehydrokavainMonoamine OxidaseJAKIKKSTATNO SynthaseCytochrome P450MAOJanus kinaseIκB kinaseI kappa B kinase Nitric oxide synthasesNOSCYPsTNF-αIL-6Inhibitorinhibitorinhibit

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