Harmine

Biological Activity

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.

Technical Data

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.

Background References

1. Recent advances in the design, synthesis, and biological evaluation of selective DYRK1A inhibitors: a new avenue for a disease modifying treatment of Alzheimer's?
   Smith et al.
   ACS Chem.Neurosci., 2012;3:857
2. The selectivity of protein kinase inhibitors: a further update.
   Bain et al.
   Biochem.J., 2007;408:297
3. A high-throughput chemical screen reveals that harmine-mediated inhibition of DYRK1A increases human pancreatic beta cell replication.
   Wang et al.
   Nat.Med., 2015;21:383
4. The small molecule harmine is an antidiabetic cell-type-specific regulator of PPARγ expression.
   Waki et al.
   Cell Metab., 2007;5:357

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