Harmine

Pricing Availability   Qty
Cat.No. 5075 - Harmine | C13H12N2O | CAS No. 442-51-3
Description: Potent and selective DYRK1A inhibitor
Chemical Name: 7-Methoxy-1-methyl-9H-pyrido[3,4-b]indole
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

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. Also induces pancreatic beta cell proliferation. Exhibits antidiabetic activity. Orally bioavailable.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

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

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

Certificate of Analysis / Product Datasheet
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References

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


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Citations for Harmine

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Literature in this Area

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