Catalog Number: 5075
Chemical Name: 7-Methoxy-1-methyl-9H-pyrido[3,4-b]indole
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
  • Solubility:
    Soluble to 100 mM in DMSO and to 5 mM in ethanol with gentle warming
  • Purity:
    >98%
  • Storage:
    Store at RT
  • CAS No:
    442-51-3
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.
Background References
  1. The selectivity of protein kinase inhibitors: a further update.
    Bain et al.
    Biochem.J., 2007;408:297
  2. 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
  3. The small molecule harmine is an antidiabetic cell-type-specific regulator of PPARγ expression.
    Waki et al.
    Cell Metab., 2007;5:357
  4. 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

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