Harmine hydrochloride

For research use only.

Catalog No.S3817 Synonyms: Telepathine hydrochloride

Harmine hydrochloride Chemical Structure

CAS No. 343-27-1

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) and cdc-like kinases (CLKs). Harmine inhibits 5-HT2A serotonin receptor with Ki of 397 nM.

Purity & Quality Control

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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) and cdc-like kinases (CLKs). Harmine inhibits 5-HT2A serotonin receptor with Ki of 397 nM.
Targets
DYRK1A [1]
(Cell-free assay)
MNB [1]
(Cell-free assay)
DYRK1B [1]
(Cell-free assay)
DYRK2 [1]
(Cell-free assay)
33 nM 149 nM 166 nM 1.9 μM
In vitro

Harmine inhibits substrate phosphorylation by DYRK1A more potently than it inhibits substrate phosphorylation by the closely related kinase DYRK1B [half maximal inhibitory concentrations (IC50) of 33 nM versus 166 nM, respectively] and by the more distant members of the family, DYRK2 and DYRK4 (1.9 μM and 80 μM, respectively). Much higher concentrations of harmine are required to suppress tyrosine autophosphorylation of the translational intermediate of DYRK1A in a bacterial in vitro translation system (IC50 = 1.9 μM). Harmine inhibits the phosphorylation of a specific substrate by DYRK1A in cultured cells with a potency similar to that observed in vitro (IC50=48 nM), without negative effects on the viability of the cells. Harmine does not inhibit tyrosine autophosphorylation of DYRK1A in HEK293 cells[1]. Harmine is able to induce beta cell proliferation, increase islet mass and improve glycemic control. It is a CNS stimulant[2].

In vivo In a partial pancreatectomy (PPX) model, harmine treatment induces Ki-67 labeling in beta cells in both sham-operated mice and in mice subjected to PPX, with the most robust proliferation in the beta cells of harmine-treated PPX mice. In the PPX model, regeneration of beta cell mass is substantially more rapid in the harmine-treated mice than in the controls, reaching near-normal values in only 14 d. In a euglycemic nonobese diabetic-severe combined immunodeficiency (NOD-SCID) mouse model, BrdU and Ki-67 labeling is two- to threefold higher in human beta cells transplanted into the renal capsule of harmine-treated compared to control euglycemic mice, without evidence of beta cell death. In a marginal mass human islet transplant model in streptozotocin-diabetic NOD-SCID mice, harmine treatment also results in near normal glycemic control. Harmine induces production of the important beta cell transcription factors NKX6.1, PDX1 and MAFA.

Protocol

Cell Research:

[1]

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  • Cell lines: HeLa and HEK293 cells
  • Concentrations: 1 nM-100 μM
  • Incubation Time: 56 h
  • Method:

    The effects of inhibitors on cell proliferation and viability are determined using a tetrazolium salt-based assay (WST-1). HeLa or HEK293 cells are seeded at a density of 5000 cells per well on 96-well plates. After overnight culture, serial dilutions of harmine in culture medium are applied to the wells (as triplicate samples) and the cells are cultured for 56 h without changing the medium, before the WST-1 assay is performed.


    (Only for Reference)
Animal Research:

[2]

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  • Animal Models: C57BL/6 mice
  • Dosages: 10 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 21 mg/mL (84.43 mM)
Water 21 mg/mL (84.43 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 248.71
Formula

C13H12N2O.HCl

CAS No. 343-27-1
Storage powder
in solvent
Synonyms Telepathine hydrochloride
Smiles CC1=NC=CC2=C1NC3=C2C=CC(=C3)OC.Cl

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID