2. Neuronal Signaling Apoptosis PI3K/Akt/mTOR
  3. Akt Monoamine Oxidase Apoptosis PI3K
  4. Osthenol

Osthenol (Ostenol) is a reversible, selective, competitive inhibitor of hMAO-A (IC50=0.74 μM, Ki=0.26 μM), with antifungal and antibacterial activity. Osthenol inhibits the oxidative deamination of hMAO-A and regulates the metabolism of monoamine neurotransmitters. Osthenol also inhibits the PI3K/AKT signaling pathway to induce apoptosis of colon cancer cells, arrest the cell cycle at the G1 phase, and inhibit cell proliferation. Osthenol is mainly used in the study of neurological diseases and cancer, especially depression-related MAO-A targeted intervention and colon cancer.

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Osthenol Chemical Structure

Osthenol Chemical Structure

CAS No. : 484-14-0

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Based on 1 publication(s) in Google Scholar

Osthenol Related Antibodies

Top Publications Citing Use of Products

View All Akt Isoform Specific Products:

View All Isoforms
Akt Akt1 Akt2 Akt3

View All Monoamine Oxidase Isoform Specific Products:

View All Isoforms
MAO-A MAO-B

View All PI3K Isoform Specific Products:

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

  • Biological Activity

  • Purity & Documentation

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Description

Osthenol (Ostenol) is a reversible, selective, competitive inhibitor of hMAO-A (IC50=0.74 μM, Ki=0.26 μM), with antifungal and antibacterial activity. Osthenol inhibits the oxidative deamination of hMAO-A and regulates the metabolism of monoamine neurotransmitters. Osthenol also inhibits the PI3K/AKT signaling pathway to induce apoptosis of colon cancer cells, arrest the cell cycle at the G1 phase, and inhibit cell proliferation. Osthenol is mainly used in the study of neurological diseases and cancer, especially depression-related MAO-A targeted intervention and colon cancer[1][2][3][4].

IC50 & Target[1]

hMAO-A

0.26 μM (Ki)

hMAO-A

0.74 μM (IC50)

Cellular Effect
Cell Line Type Value Description References
Neutrophil IC50
> 10 μM
Compound: 16
Antiinflammatory activity in human neutrophil assessed as inhibition of FMLP/CB-induced elastase release for 5 mins
Antiinflammatory activity in human neutrophil assessed as inhibition of FMLP/CB-induced elastase release for 5 mins
[PMID: 24798144]
Neutrophil IC50
2.6 μM
Compound: 16
Antiinflammatory activity in human neutrophil assessed as inhibition of FMLP/CB-induced superoxide anion generation pretreated for 5 mins by spectrophotometry
Antiinflammatory activity in human neutrophil assessed as inhibition of FMLP/CB-induced superoxide anion generation pretreated for 5 mins by spectrophotometry
[PMID: 24798144]
In Vitro

Osthenol (0.74 μM; enzyme activity assay) exhibits potent, selective and reversible competitive inhibitory activity against recombinant hMAO-A with IC50=0.74 μM, SI >81.1[1].
Osthenol (25-100 μM; 24-48 h) significantly inhibits cell proliferation, induces apoptosis, arrests the cell cycle at the G1 phase and inhibits cell migration in HCT116 human colon cancer cells assay[2].
Osthenol has antifungal activity with MICs of 125 μg/mL against Fusarium solani and 250 μg/mL against Candida albicans and Aspergillus fumigatus[3].
Osthenol is effective against Gram-positive bacteria with MICs of 125-62.5 μg/mL[4].

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

Osthenol Related Antibodies

Apoptosis Analysis[2]

Cell Line: Apoptosis Assay (HCT116 Cells) HCT116
Concentration: 25-100 μM
Incubation Time: 48 h
Result: Total apoptotic cells rose from 7.06% (control) to 30.12% (25 μM), 33.11% (50 μM), and 52.5% (100 μM).
Dose-dependently increased the activation of caspase-3, -8, and -9 (cleaved caspase levels increasing).
In Vivo

Osthenol (5 mg/kg; intravenous injection; single dose) has a rapid distribution characteristic in male ICR mice, with initial blood concentration C0=14.3 μg/mL, T1/2=47.0 min, AUClast=211.5 μg·min/mL, MRTlast=22.5 min[5].
Osthenol (5 mg/kg, 20 mg/kg; oral gavage; single dose) has extremely low bioavailability in male ICR mice (0.43% and 0.02%, respectively), and is rapidly metabolized to sulfonylated (M1) and glucuronidated (M2) conjugates after oral administration[5].

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

230.26

Formula

C14H14O3
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

O=C1C=CC2=CC=C(O)C(C/C=C(C)\C)=C2O1
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 : 100 mg/mL (434.29 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 4.3429 mL 21.7146 mL 43.4292 mL
5 mM 0.8686 mL 4.3429 mL 8.6858 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)

Mass
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Concentration
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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)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

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 (10.86 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    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 (10.86 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:

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).
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: 99.27%

SDS (251 KB)

COA (250 KB) HNMR (244 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 4.3429 mL 21.7146 mL 43.4292 mL 108.5729 mL
5 mM 0.8686 mL 4.3429 mL 8.6858 mL 21.7146 mL
10 mM 0.4343 mL 2.1715 mL 4.3429 mL 10.8573 mL
15 mM 0.2895 mL 1.4476 mL 2.8953 mL 7.2382 mL
20 mM 0.2171 mL 1.0857 mL 2.1715 mL 5.4286 mL
25 mM 0.1737 mL 0.8686 mL 1.7372 mL 4.3429 mL
30 mM 0.1448 mL 0.7238 mL 1.4476 mL 3.6191 mL
40 mM 0.1086 mL 0.5429 mL 1.0857 mL 2.7143 mL
50 mM 0.0869 mL 0.4343 mL 0.8686 mL 2.1715 mL
60 mM 0.0724 mL 0.3619 mL 0.7238 mL 1.8095 mL
80 mM 0.0543 mL 0.2714 mL 0.5429 mL 1.3572 mL
100 mM 0.0434 mL 0.2171 mL 0.4343 mL 1.0857 mL
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Osthenol 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:

Osthenol484-14-0OstenolAktMonoamine OxidaseApoptosisPI3KPKBProtein kinase BMAOPhosphoinositide 3-kinasecoumarinselectivecompetitivedepressionInhibitorinhibitorinhibit

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