Biological Activity
Selective inhibitor of p38α and p38β2 that displays no activity at p38γ, p38δ, ERK1/2 and JNK1. Inhibits production of inflammatory cytokines including IL-8, TNF-α, IL-6, IL-1β and IL-10 (IC50 values are 4, 5, 17, 30 and 74 nM respectively). Displays anti-inflammatory activity in murine models of acute and chronic dermatitis.
Compound Libraries
EO 1428 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 415.71 |
| Formula | C20H16BrClN2O |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 321351-00-2 |
| PubChem ID | 9801969 |
| InChI Key | HDCLCHNAEZNGNV-UHFFFAOYSA-N |
| Smiles | CC1=CC=CC=C1C(C2=CC=C(NC3=C(N)C=C(Br)C=C3)C=C2Cl)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 41.57 | 100 | |
| ethanol | 20.79 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 415.71. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.41 mL | 12.03 mL | 24.06 mL |
| 5 mM | 0.48 mL | 2.41 mL | 4.81 mL |
| 10 mM | 0.24 mL | 1.2 mL | 2.41 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.48 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Ottosen et al (2003) Synthesis and structure-activity relationship of aminobenzophenones. A novel class of p38 MAP kinase inhibitors with high antiinflammatory activity. J.Med.Chem. 46 5651 PMID: 14667219
Keywords: EO 1428, supplier, Selective, inhibitors, inhibits, p38α, p38alpha, p38β2, p38β, p38beta2, MAPK, Signaling, Signalling, Mitogen-Activated, Protein, Kinases, EO1428, p38, p38, Tocris Bioscience
