Home Metabolism PPAR modulator - MAO inhibitor Harmine For research use only.

Harmine

Synonyms: Telepathine

Harmine (Telepathine), a fluorescent harmala alkaloid belonging to the beta-carboline family of compounds, is a highly cell-permeant and competitive inhibitor of ATP binding to the kinase pocket of DYRK1A, with about 60-fold higher IC50 value for DYRK2. Harmine also inhibits monoamine oxidases (MAOs), PPARγ and cdc-like kinases (CLKs). Harmine inhibits 5-HT2A serotonin receptor with Ki of 397 nM.

Harmine Chemical Structure

Harmine Chemical Structure

CAS No. 442-51-3

Purity & Quality Control

Harmine Related Products

Signaling Pathway

PPAR Signaling Pathways

PPAR Signaling Pathway

Biological Activity

Description Harmine (Telepathine), a fluorescent harmala alkaloid belonging to the beta-carboline family of compounds, is a highly cell-permeant and competitive inhibitor of ATP binding to the kinase pocket of DYRK1A, with about 60-fold higher IC50 value for DYRK2. Harmine also inhibits monoamine oxidases (MAOs), PPARγ and cdc-like kinases (CLKs). Harmine inhibits 5-HT2A serotonin receptor with Ki of 397 nM.
Targets
PPARγ [1] MAO-A [2]
(Cell-free assay)
0.048 μM(Ki)
In vitro
In vitro Harmine does not cause significant weight gain or hepatic lipid accumulation. Harmine induces expression of both PPARγ1 and PPARγ2 in primary mouse bone-marrow-derived macrophages. It might promote the anti-inflammatory action of PPARγ in this cell type. Harmine has previously been reported to interact with several cell-surface receptors, including monoamine oxidase A (MAO-A), serotonin receptor 2A (5-HT2A), imidazoline receptors (I1 and I2 sites), and cyclin-dependent kinases[1]. Harmine has also been reported as a potent inhibitor of the dual specificity tyrosine-phosphorylation-regulated kinase (DYRK1A), which regulates cell proliferation and brain development. In fact, harmine also inhibits DYRK1B and DYRK2, but the efficiency of this inhibition is, respectively, 5- and 50-fold lower in comparison to DYRK1A. Harmine can increase proliferation of human neural progenitors[2].
Cell Research Cell lines Human neural progenitor cells
Concentrations --
Incubation Time 4 days
Method Cell proliferation, cell death and DNA damage experiments are performed in a High Content Screening (HCS) format. The hNPCs (1,500 cells/per well) are plated on a multiwell 384 µClear plate coated with 100 µg/mL Poly-L-ornithine and 10 µg/mL laminin. After 24 h, cells are treated for 4 days in quintuplicate (five wells per condition) with harmine, INDY and pargyline in N2B27 medium supplemented with bFGF and EGF. On day 4 cells are labelled with 10 µM EdU for 2 h (cell proliferation) or BOBO™-3 (cell death) for 30 min prior to fixation or image acquisition, respectively.
In Vivo
In vivo Administration of harmine to diabetic mice mimics the effects of PPARγ ligands on adipocyte gene expression and insulin sensitivity. Harmine does not cause significant weight gain or hepatic lipid accumulation. It regulates metabolic and inflammatory gene expression in vivo[1]. Harmaline exhibits a dose-dependent bioavailability[2].
Animal Research Animal Models C57BL/6 mice
Dosages 30 mg/kg
Administration i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06252506 Recruiting
Neuropharmacological Investigation of Ayahuasca Constituents DMT and Harmine
Insel Gruppe AG University Hospital Bern|Psychiatric University Hospital Zurich
 January 22 2024 Phase 1

Chemical Information & Solubility

Molecular Weight 212.25 Formula

C13H12N2O
CAS No. 442-51-3 SDF --
Smiles CC1=NC=CC2=C1NC3=C2C=CC(=C3)OC
Storage (From the date of receipt)

In vitro
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DMSO : 42 mg/mL ( (197.87 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)


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