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AMG-548 dihydrochloride is an orally active, selective inhibitor of p38α (Ki=0.5 nM), slightly selective for p38β (Ki=36 nM), and >1000-fold selective for p38γ and p38δ. AMG-548 dihydrochloride also potently inhibits whole blood LPS-stimulated TNFα (IC50=3 nM). LPS-stimulated TNFα (IC50=3 nM). In addition, AMG-548 dihydrochloride inhibits Wnt signaling through direct inhibition of Casein kinase 1 isoforms δ and ε.
| Molecular Weight | 534.48 |
| Formula | C29H29Cl2N5O |
| CAS Number | 2518299-32-4 |
| Form | Solid |
| Solubility (25°C) | DMSO 10 mg/mL |
| Storage | -20°C, dry, sealed |
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