Chemical Name:4-[4-(2,3-Dihydro-1,4-benzodioxin-6-yl)-5-(2-pyridinyl)
-1H-imidazol-2-yl]benzamide
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.
Callahanet al
(2002) Identification of novel inhibitors of the transforming growth factor β1 (TGF-β1) type I receptor (ALK5).
J.Med.Chem. 45 999. Renaet al (2004) D4476, a
cell-permeant inhibitor of CK1, suppresses the site-specific phosphorylation
and nuclear exclusion of FOXO1a. EMBO Rep. 5 60. Bainet
al (2007) The selectivity of protein kinase inhibitors: a further update.
Biochem.J. 408 297.