Casein Kinase I Inhibitor, D4476-CAS 301836-43-1-Calbiochem

C₂₃H₁₈N₄O₃

398.41

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).

Cell permeable: yes
Target IC₅₀: 0.2 µM against CK1 from S. pombe; 0.3 µM for CK1δ 0.5 µM against ALK5
Product competes with ATP.
Reversible: yes

Toxicity: Standard Handling (A)

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

100

≥95% (HPLC)

crystalline solid

Calbiochem^®

OK to freeze
protect from light

DMSO: 40 mg/mL

ambient

2-8℃

1 mg in Plastic ampoule
Packaged under inert gas