General Description
A cell-permeable, potent, and relatively specific ATP-competitive inhibitor of CK1 (IC
50 = 200 nM from
S. pombe; 0.3 μM for CK1δ) and ALK5 (IC
50 = 500 nM). A weak inhibitor of p38α MAP kinase (IC
50 = 12 μM) and several other kinases tested, including PKB, SGK, and GSK-3β. Suppresses the site-specific phosphorylation (Ser
322 and Ser
325) and nuclear exclusion of FOXO1A in H4IIE hepatoma cells. Shown to be ~10-fold more potent than IC261 (Cat. No. 400090; IC
50 = 2.5 μM for CK1).
Biochem/physiol Actions
Target IC50: 0.2 μM, 0.3 μM against CK1, CK1d, respectively
