Harmine hydrochloride

製品コードS3817 バッチS381702

印刷

化学情報

Chemical Structure Synonyms Telepathine hydrochloride Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C13H12N2O.HCl
分子量 248.71 CAS No. 343-27-1
Solubility (25°C)* 体外  
 
 
* <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.

生物活性

製品説明 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.
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.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 HeLa and HEK293 cells
濃度 1 nM-100 μM
反応時間 56 h
実験の流れ

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.
動物実験 動物モデル C57BL/6 mice
投薬量 10 mg/kg
投与方法 i.p.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

CRISPR-Cas9 Screen Identifies DYRK1A as a Target for Radiotherapy Sensitization in Pancreatic Cancer [ Cancers (Basel), 2022, 14(2)326] PubMed: 35053488

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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