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 | |||
| DMSO | 21.23 | 100 | |
| ethanol | 1.06 | 5mM with gentle warming |
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 |
Molarity Calculator
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Product Datasheets
References
References are publications that support the products' biological activity.
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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