Biological Activity
Selective inhibitor of casein kinase 1 (CK1) and TGF-β type-I receptor (ALK5) that displays > 20-fold selectivity over SAPK2/p38 and a much greater selectivity over all other protein kinases tested. Suppresses site-specific phosphorylation and nuclear exclusion of FOXO1a.
Licensing Information
Sold with the permission of GlaxoSmithKline
Compound Libraries
D 4476 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 398.41 |
| Formula | C23H18N4O3 |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 301836-43-1 |
| PubChem ID | 6419753 |
| InChI Key | DPDZHVCKYBCJHW-UHFFFAOYSA-N |
| Smiles | O=C(N)C4=CC=C(C=C4)C1=NC(C2=CC(OCCO5)=C5C=C2)=C(C3=NC=CC=C3)N1 |
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 | 39.84 | 100 | |
| ethanol | 19.92 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 398.41. 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 | 2.51 mL | 12.55 mL | 25.1 mL |
| 5 mM | 0.5 mL | 2.51 mL | 5.02 mL |
| 10 mM | 0.25 mL | 1.25 mL | 2.51 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.5 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Callahan et al (2002) Identification of novel inhibitors of the transforming growth factor β1 (TGF-β1) type I receptor (ALK5). J.Med.Chem. 45 999 PMID: 11855979
Rena et al (2004) D4476, a cell-permeant inhibitor of CK1, suppresses the site-specific phosphorylation and nuclear exclusion of FOXO1a. EMBO Rep. 5 60 PMID: 14710188
Bain et al (2007) The selectivity of protein kinase inhibitors: a further update. Biochem.J. 408 297 PMID: 17850214
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