218696
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
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EMD Chemicals, Inc.
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24 May 2012
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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).
| Product information | |||
|---|---|---|---|
| Form | Crystalline solid | ||
| Primary Target | CK1, CK1d | ||
| Primary Target IC50 | 0.2 µM, 0.3 µM | ||
| Secondary target | ALK5 (IC50 = 0.5 µM), p38a MAP kinase (IC50 = 12 µM) | ||
| Molar mass | 398.4 | ||
| Protect from Light | Yes | ||
| Packaged under inert gas | Yes | ||
| Cell permeable | Yes | ||
| ATP Competitive | Yes | ||
| Purity | ≥95% by HPLC | ||
| Solubility | DMSO | ||
| Chemical formula | C23H18N4O3 | ||
| CAS number | 301836-43-1 | ||
| Store and ship information | |||
|---|---|---|---|
| Storage | +2°C to +8°C | ||
| Ship |
Ambient Temperature Only
Standard Handling |
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