Biological Activity
High affinity and selective p38 kinase inhibitor (Kd = 50-100 pM). Exhibits no significant inhibition on a panel of related kinases. Inhibits LPS-induced TNFα production in human PBMCs and whole blood (IC50 values are 21 and 960 nM, respectively). Also inhibits JNK2α2 and c-Raf-1 (IC50 values are 98 nM and 1.4 μM, respectively). Cell permeable.
Technical Data
| M. Wt | 527.66 |
| Formula | C31H37N5O3 |
| Storage | Store at -20°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 285983-48-4 |
| PubChem ID | 156422 |
| InChI Key | MVCOAUNKQVWQHZ-UHFFFAOYSA-N |
| Smiles | CC1=CC=C(N2N=C(C(C)(C)C)C=C2NC(NC3=CC=C(C4=C3C=CC=C4)OCCN5CCOCC5)=O)C=C1 |
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 | 52.77 | 100 | |
| ethanol | 26.38 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 527.66. 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 | 1.9 mL | 9.48 mL | 18.95 mL |
| 5 mM | 0.38 mL | 1.9 mL | 3.79 mL |
| 10 mM | 0.19 mL | 0.95 mL | 1.9 mL |
| 50 mM | 0.04 mL | 0.19 mL | 0.38 mL |
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References
References are publications that support the products' biological activity.
Laufer et al (2008) Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region. J.Med.Chem. 51 4122 PMID: 18578517
Regan et al (2003) Structure-activity relationships of the p38alpha MAP kinase inhibitor 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naph- thalen-1-yl]urea (BIRB 796). J.Med.Chem. 46 4676 PMID: 14561087
Goldstein et al (2010) Selective p38α inhibitors clinically evaluated for the treatment of chronic inflammatory disorders. J.Med.Chem. 53 2345 PMID: 19950901
Kuma et al (2005) BIRB796 inhibits all p38 MAPK isoforms in vitro and in vivo. J.Biol.Chem. 280 19472 PMID: 15755732
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