Biological Activity
Potent, ATP-competitive inhibitor of Clk-family kinases (IC50 values are 15, 20 and 200 nM for mClk4, 1 and 2 respectively and >10 μM for mClk3). Also inhibits DYRK1A/B (IC50 values are 24 and 34 nM respectively). Suppresses serine/arginine-rich protein phosphorylation; affects the regulation of alternative splicing by phosphorylation of SR protein both in vitro and in vivo.
Technical Data
| M. Wt | 249.33 |
| Formula | C13H15NO2S |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 719277-26-6 |
| PubChem ID | 647991 |
| InChI Key | BGVLELSCIHASRV-UHFFFAOYSA-N |
| Smiles | O=C(C)/C=C1SC2=CC=C(OC)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 | 24.93 | 100 | |
| ethanol | 18.7 | 75 |
Preparing Stock Solutions
The following data is based on the product molecular weight 249.33. 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 | 4.01 mL | 20.05 mL | 40.11 mL |
| 5 mM | 0.8 mL | 4.01 mL | 8.02 mL |
| 10 mM | 0.4 mL | 2.01 mL | 4.01 mL |
| 50 mM | 0.08 mL | 0.4 mL | 0.8 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Muraki et al (2004) Manipulation of alternative splicing by a newly developed inhibitor of Clks. J.Biol.Chem. 279 24246 PMID: 15010457
Foucourt et al (2014) Design and synthesis of thiazolo[5,4-f]quinazolines as DYRK1A inhibitors, part II. Molecules 19 15411 PMID: 25264830
Keywords: TG 003, supplier, TG003, ATP-competitive, Cdc2-like, inhibitors, inhibits, Clk, Clk-family, kinases, DYRK1A, DYRK1B, DYRK1A/B, Cdc2-like, kinases, DYRK, Cdc2-like, kinases, Tocris Bioscience
