Description: Selective CK1 inhibitor. Also inhibits TGF-βRI
Chemical Name: 4-[4-(2,3-Dihydro-1,4-benzodioxin-6-yl)-5-(2-pyridinyl)-1H-imidazol-2-yl]benzamide
Purity: ≥99% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
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.
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
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Callahanet 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
Renaet 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
Bainet al (2007) The selectivity of protein kinase inhibitors: a further update. Biochem.J. 408 297 PMID: 17850214