Casein Kinase I Inhibitor; D4476

Biochem/physiol Actions

Reversible: yes

Product competes with ATP.

Target IC₅₀: 0.2 µM against CK1 from S. pombe; 0.3 µM for CK1δ 0.5 µM against ALK5

Cell permeable: yes

General description

A cell-permeable triaryl substituted imidazolo compound that acts as a potent, reversible and relatively specific ATP-competitive inhibitor of CK1 (IC₅₀ = 0.2 µM from S. pombe; 0.3 µM for CK1δ) and ALK5 (IC₅₀ = 0.5 µM). A weak inhibitor of p38α MAP kinase (IC₅₀ = 12 µM) and only weakly affects the activities of a panel of kinases tested, including PKB, SGK and GSK-3β. Suppresses the site-specific phosphorylation (Ser³²² and Ser³²⁵) and nuclear exclusion of FOXO1a in H4IIE hepatoma cells. Shown to be ~10-fold more potent than IC261 (Cat. No. 400090; IC₅₀ = 2.5 µM for CK1).

A cell-permeable, reversible, potent, and relatively specific ATP-competitive inhibitor of CK1 (IC₅₀ = 200 nM from S. pombe; 0.3 µM for CK1δ) and ALK5 (IC₅₀ = 500 nM). A weak inhibitor of p38α MAP kinase (IC₅₀ = 12 µM) and several other kinases tested, including PKB, SGK, and GSK-3β. Suppresses the site-specific phosphorylation (Ser³²² and Ser³²⁵) and nuclear exclusion of FOXO1A in H4IIE hepatoma cells. Shown to be ~ 10-fold more potent than IC261 (Cat. No. 400090; IC₅₀ = 2.5 µM for CK1).

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Packaging

1 mg in Plastic ampoule

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)