Harmine

Catalog No.S3868 Synonyms: telepathine

Harmine Chemical Structure

Molecular Weight(MW): 212.25

Harmine is an alkaloid of the β-carboline family that regulates PPARγ expression through inhibition of the Wnt signaling pathway. It also selectively binds to MAO-A and reversibly inhibits monoamine oxidase A (MAO-A) but not the variant MAO-B.

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Description Harmine is an alkaloid of the β-carboline family that regulates PPARγ expression through inhibition of the Wnt signaling pathway. It also selectively binds to MAO-A and reversibly inhibits monoamine oxidase A (MAO-A) but not the variant MAO-B.
Targets
PPARγ [1]
()
MAO-A [2]
(Cell-free assay)
0.048 μM(Ki)
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].

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].

Protocol

Cell Research:[2]
+ Expand
  • 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.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: C57BL/6 mice
  • Formulation: saline
  • Dosages: 30 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 42 mg/mL (197.87 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 212.25
Formula

C13H12N2O

CAS No. 442-51-3
Storage powder
in solvent
Synonyms telepathine

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PPAR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID