Harmine

Product Description

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 (K_d = 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.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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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

Calculators

Background References

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

• Li The yjdF riboswitch candidate regulates gene expression by binding diverse azaaromatic compounds. RNA 2016 PMID: 26843526
• Wang A high-throughput chemical screen reveals that harmine-mediated inhibition of DYRK1A increases human pancreatic beta cell replication. Nat.Med. 2015 PMID: 25751815
• Bain The selectivity of protein kinase inhibitors: a further update. Biochem.J. 2007 PMID: 17850214
• Waki The small molecule harmine is an antidiabetic cell-type-specific regulator of PPARγ expression. Cell Metab. 2007 PMID: 17488638
• Smith 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. 2012 PMID: 23173067