218705

Casein Kinase I Inhibitor, D4476

InSolution, ≥95%

• Synonym(s): InSolution Casein Kinase I Inhibitor, D4476
• Empirical Formula (Hill Notation): C₂₃H₁₈N₄O₃
• Molecular Weight: 398.41
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥95% (HPLC)
• form: liquid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; desiccated (hygroscopic); protect from light
• shipped in: wet ice
• storage temp.: −20°C

Description

General description

A cell-permeable, 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).

Biochem/physiol Actions

Cell permeable: yes

Primary Target
CK1, CK1d

Product competes with ATP.

Reversible: no

Target IC₅₀: 0.2 µM, 0.3 µM against CK1, CK1d, respectively

Packaging

Packaged under inert gas

Please refer to vial label for lot-specific concentration.

Warning

Toxicity: Irritant (B)

Physical form

A 10 mM (1 mg/251 µl) solution of Casein Kinase I Inhibitor, D4476 (Cat. No. 218696) in DMSO

Reconstitution

Following initial use, aliquot and refrigerate (4°C).

Other Notes

Rena, G., et al. 2004. EMBO Reports5, 60.

Legal Information

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