Harmine

Catalog No.S3868 Batch:S386801

Technical Data

Formula	C₁₃H₁₂N₂O
Molecular Weight	212.25	CAS No.	442-51-3
Solubility (25°C)*	In vitro	DMSO	42 mg/mL (197.87 mM)


* <1 mg/ml means slightly soluble or insoluble. * 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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 (from reference)

Cell Assay:^{^[2]}	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.
Animal Study:^{^[1]}	Animal Models C57BL/6 mice Dosages 30 mg/kg Administration i.p.

Cell Assay:^{^[2]}

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.

Animal Study:^{^[1]}

Animal Models
C57BL/6 mice
Dosages
30 mg/kg
Administration
i.p.

References

Selleck's Harmine has been cited by 2 publications

Screening Health-Promoting Compounds for Their Capacity to Induce the Activity of FOXO3 [ J Gerontol A Biol Sci Med Sci, 2022, 77-8:1485-1493]	PubMed: 34508571
MKL1 promotes endothelial-to-mesenchymal transition and liver fibrosis by activating TWIST1 transcription. [ Cell Death Dis, 2019, 10(12):899]	PubMed: 31776330

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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