Harmine

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Description: Potent and selective DYRK1A inhibitor
Chemical Name: 7-Methoxy-1-methyl-9H-pyrido[3,4-b]indole
Purity: ≥98% (HPLC)
Datasheet
Citations (1)
Reviews
Literature (4)

Biological Activity for Harmine

Harmine is a potent and selective inhibitor of DYRK1A (IC50 values are 80, 800 and 900 nM for DYRK1A, DYRK3 and DYRK2 respectively). Inhibits DYRK1A-mediated tau phosphorylation and regulates PPARγ expression. Harmine also induces pancreatic β cell proliferation and exhibits antidiabetic activity. Orally bioavailable. Harmine has high affinity (Kd = 100 nM) for the yjdF aptamer. The riboswitch function of yjdF motif RNAs is activated by Harmine and leads to robust reporter gene expressions in B. subtilis.

Technical Data for Harmine

M. Wt 212.25
Formula C13H12N2O
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 442-51-3
PubChem ID 5280953
InChI Key BXNJHAXVSOCGBA-UHFFFAOYSA-N
Smiles CC1=NC=CC2=C1NC3=C2C=CC(OC)=C3

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Harmine

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 21.23 100
ethanol 1.06 5 with gentle warming

Preparing Stock Solutions for Harmine

The following data is based on the product molecular weight 212.25. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 4.71 mL 23.56 mL 47.11 mL
5 mM 0.94 mL 4.71 mL 9.42 mL
10 mM 0.47 mL 2.36 mL 4.71 mL
50 mM 0.09 mL 0.47 mL 0.94 mL

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Product Datasheets for Harmine

Certificate of Analysis / Product Datasheet
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References for Harmine

References are publications that support the biological activity of the product.

Smith et al (2012) Recent advances in the design, synthesis, and biological evaluation of selective DYRK1A inhibitors: a new avenue for a disease modifying treatment of Alzheimer's? ACS Chem.Neurosci. 3 857 PMID: 23173067

Bain et al (2007) The selectivity of protein kinase inhibitors: a further update. Biochem.J. 408 297 PMID: 17850214

Waki et al (2007) The small molecule harmine is an antidiabetic cell-type-specific regulator of PPARγ expression. Cell Metab. 5 357 PMID: 17488638

Wang et al (2015) A high-throughput chemical screen reveals that harmine-mediated inhibition of DYRK1A increases human pancreatic beta cell replication. Nat.Med. 21 383 PMID: 25751815

Li et al (2016) The yjdF riboswitch candidate regulates gene expression by binding diverse azaaromatic compounds. RNA 22 530 PMID: 26843526


If you know of a relevant reference for Harmine, please let us know.

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View all DYRK Inhibitors

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1 Citation for Harmine

Citations are publications that use Tocris products. Selected citations for Harmine include:

Singh et al (2017) Different developmental histories of beta-cells generate functional and proliferative heterogeneity during islet growth. Nat Commun 8 664 PMID: 28939870


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Reviews for Harmine

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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