Cat. No. 5075
Chemical Name: 7-Methoxy-1-methyl-9H-pyrido[3,4-b]
Biological ActivityPotent 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.
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.
Certificate of Analysis / Product Datasheet / Safety Data Sheet
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.
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.
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Keywords: Harmine, supplier, Harmine, dyrk1a, dyrk, inhibitors, inhibits, potent, selective, dual, specificity, tyrosine, phosphorylation, regulated, kinase-1A, PPARg, PPARgamma, PPARγ, antidiabetic, Tocris Bioscience, DYRK Inhibitor products
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