1. Protein Tyrosine Kinase/RTK Neuronal Signaling GPCR/G Protein
  2. DYRK 5-HT Receptor
  3. Harmine

Harmine  (Synonyms: Telepathine)

Cat. No.: HY-N0737A Purity: 99.88%
COA Handling Instructions

Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2A serotonin receptor, with an Ki of 397 nM.

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

Harmine Chemical Structure

Harmine Chemical Structure

CAS No. : 442-51-3

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 66 In-stock
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10 mM * 1 mL in DMSO USD 66 In-stock
Solid
500 mg USD 60 In-stock
1 g USD 95 In-stock
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Customer Review

Based on 17 publication(s) in Google Scholar

Other Forms of Harmine:

Top Publications Citing Use of Products

    Harmine purchased from MedChemExpress. Usage Cited in: Prog Neuropsychopharmacol Biol Psychiatry. 2017 Jun 15;79(Pt B):258-267.  [Abstract]

    Representative images showing the restoration effect of Harmine on CUS-induced decrease in hippocampal DCX protein expressions. The Fluoxetine administration (20 mg/kg) is used as a positive control, and all data are shown as mean±SEM.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2A serotonin receptor, with an Ki of 397 nM[1].

    IC50 & Target[1][2]

    5-HT2A Receptor

    397 nM (Ki)

    DYRK1A

     

    In Vitro

    Harmine inhibits tau phosphorylation by DYRK1A by selected DANDYs, with an IC50 of 190 nM[2].Harmine negatively regulates homologous recombination (HR) by interfering Rad51 recruitment, resulting in severe cytotoxicity in hepatoma cells. Furthermore, NHEJ inhibitor Nu7441 markedly sensitizes Hep3B cells to the anti-proliferative effects of Harmine[3].

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

    In Vivo

    It is shown that brain water content is significantly increased in the TBI group. Treatment with Harmine significantly reduces the tissue water content at 1, 3 and 5 days, compared with the TBI group. Harmine treatment significantly reduces the escape latency at 3 and 5 days, compared with the TBI group. Post-TBI administration of Harmine significantly improves the motor function recovery of the rats at 1, 3 and 5 days following TBI, compared with the TBI group without Harmine treatment. The neuronal survival rate in the Harmine-treated group is significantly increased, compared with the TBI group. Administration of Harmine results in marked elevation in the expression of GLT-1, compared with the TBI group. The administration of Harmine significantly reduces the expression of caspase 3, compared with the TBI group[4].

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

    Clinical Trial
    Molecular Weight

    212.25

    Formula

    C13H12N2O

    CAS No.
    Appearance

    Solid

    Color

    White to khaki

    SMILES

    CC1=NC=CC2=C1NC3=C2C=CC(OC)=C3

    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 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 30 mg/mL (141.34 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 4.7114 mL 23.5571 mL 47.1143 mL
    5 mM 0.9423 mL 4.7114 mL 9.4229 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, 1 years; -20°C, 6 months. When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

    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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    Volume (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    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (11.78 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% Corn Oil

      Solubility: ≥ 2.5 mg/mL (11.78 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

    mg/kg

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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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: 99.88%

    References
    Animal Administration
    [4]

    Rats[4]
    A total of 150 male Sprague-Dawley rats (age, 10-12 weeks; weighing, 280-320 g; are used in the present study. The rats are randomly divided into three groups: Sham-operated group (sham; n=15); the TBI group (TBI; n=35) and the TBI + Harmine-treated group (Harmine; n=35). Harmine is administered immediately following TBI (i.p, 30 mg/kg per day) for up to 5 days. The sham and TBI groups receive equal volumes of 0.9% saline solution (i.p.). The rats are grouped as follows for examination of behavioral recovery: Sham, n=3; TBI, n=7; and Harmine, n=7. Following TBI, the NSS is evaluated at 1, 3 and 5 days. Each rat is assessed by an observer who is blinded to the animal treatment[4].

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

    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, 1 years; -20°C, 6 months. When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 4.7114 mL 23.5571 mL 47.1143 mL 117.7856 mL
    5 mM 0.9423 mL 4.7114 mL 9.4229 mL 23.5571 mL
    10 mM 0.4711 mL 2.3557 mL 4.7114 mL 11.7786 mL
    15 mM 0.3141 mL 1.5705 mL 3.1410 mL 7.8524 mL
    20 mM 0.2356 mL 1.1779 mL 2.3557 mL 5.8893 mL
    25 mM 0.1885 mL 0.9423 mL 1.8846 mL 4.7114 mL
    30 mM 0.1570 mL 0.7852 mL 1.5705 mL 3.9262 mL
    40 mM 0.1178 mL 0.5889 mL 1.1779 mL 2.9446 mL
    50 mM 0.0942 mL 0.4711 mL 0.9423 mL 2.3557 mL
    60 mM 0.0785 mL 0.3926 mL 0.7852 mL 1.9631 mL
    80 mM 0.0589 mL 0.2945 mL 0.5889 mL 1.4723 mL
    100 mM 0.0471 mL 0.2356 mL 0.4711 mL 1.1779 mL
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    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.

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    Product Name:
    Harmine
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