218696

Casein Kinase I Inhibitor, D4476

The Casein Kinase I Inhibitor, D4476, also referenced under CAS 301836-43-1, controls the biological activity of Casein Kinase I. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonym(s): Casein Kinase I Inhibitor, D4476, CK1 Inhibitor, 4-(4-(2,3-Dihydrobenzo[1,4]dioxin-6-yl)-5-pyridin-2-yl-1H-imidazol-2-yl)benzamide
• Empirical Formula (Hill Notation): C₂₃H₁₈N₄O₃
• CAS Number: 301836-43-1
• Molecular Weight: 398.41
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥95% (HPLC)
• form: crystalline solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• solubility: DMSO: 40 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• InChI: 1S/C23H18N4O3/c24-22(28)14-4-6-15(7-5-14)23-26-20(21(27-23)17-3-1-2-10-25-17)16-8-9-18-19(13-16)30-12-11-29-18/h1-10,13H,11-12H2,(H2,24,28)(H,26,27)
• InChI key: DPDZHVCKYBCJHW-UHFFFAOYSA-N

Description

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).

Biochem/physiol Actions

Cell permeable: yes

Product competes with ATP.

Reversible: yes

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

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Legal Information

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable