Biological Activity
DYRK1A/B inhibitor (IC50 values are 0.23 and 0.24 μM, for DYRK1B and DYRKA respectively). Binds at the ATP-binding cleft of the enzyme. Reverses aberrant tau-phosphorylation and rescues repressed calcineurin/NFAT signaling. Impairs the self-renewal capacity of subventricular zone neural stem cells. Also available as a prodrug, proINDY (Cat. No. 4998).
Technical Data
| M. Wt | 235.3 |
| Formula | C12H13NO2S |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1169755-45-6 |
| PubChem ID | 69538603 |
| InChI Key | GCSZJMUFYOAHFY-UHFFFAOYSA-N |
| Smiles | O=C(C)/C=C1SC2=CC=C(O)C=C2N1CC |
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 | 23.53 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 235.3. 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 | 4.25 mL | 21.25 mL | 42.5 mL |
| 5 mM | 0.85 mL | 4.25 mL | 8.5 mL |
| 10 mM | 0.42 mL | 2.12 mL | 4.25 mL |
| 50 mM | 0.08 mL | 0.42 mL | 0.85 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Pozo et al (2013) Inhibition of DYRK1A destabilizes EGFR and reduces EGFR-dependent glioblastoma growth. J.Clin.Invest. 123 2475 PMID: 23635774
Ogawa et al (2010) Development of a novel selective inhibitor of the Down syndrome-related kinase Dyrk1A. Nat.Commun. 1 86 PMID: 20981014
Keywords: INDY, supplier, INDY, downs, syndrome-related, kinase, Dyrk1A/B, inhibitors, inhibits, tau, phosphorylation, hyperphosphorylation, calcineurin, NFAT, signalling, self-renewal, neural, stem, cells, NSCs, Microtubules, Stem, Cell, Proliferation, DYRK, DYRK, Tocris Bioscience
