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: 99.93%
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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10 mM * 1 mL in DMSO USD 66 In-stock
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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Harmine:

Top Publications Citing Use of Products

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

    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.
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    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]

    DYRK1A

     

    5-HT2A Receptor

    397 nM (Ki)

    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].

    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].

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

    Molecular Weight

    212.25

    Formula

    C₁₃H₁₂N₂O

    CAS No.

    442-51-3

    SMILES

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

    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 : 12.5 mg/mL (58.89 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    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
    10 mM 0.4711 mL 2.3557 mL 4.7114 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (11.78 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    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

    Purity: 99.93%

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    Keywords:

    HarmineTelepathineDYRK5-HT ReceptorDual specificity tyrosine phosphorylation regulated kinaseDual specificity tyrosine regulated kinaseSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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