Biological Activity
Selective p38α and p38β inhibitor (IC50 values are 1 and 11 μM respectively) that displays no activity at p38γ, p38δ and a range of other kinases. Potently inhibits TNF-α and IL-1β release (IC50 values are 3 and 11 nM respectively) and suppresses HIV-1 replication in T cells in vitro. Displays cardioprotective and anti-inflammatory activity in vivo. Orally active.
Compound Libraries
RWJ 67657 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 | 425.5 |
| Formula | C27H24FN3O |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 215303-72-3 |
| PubChem ID | 3008319 |
| InChI Key | QSUSKMBNZQHHPA-UHFFFAOYSA-N |
| Smiles | FC(C=C4)=CC=C4C(N=C(C#CCCO)N2CCCC3=CC=CC=C3)=C2C1=CC=NC=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 | 42.55 | 100 | |
| ethanol | 42.55 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 425.5. 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 | 2.35 mL | 11.75 mL | 23.5 mL |
| 5 mM | 0.47 mL | 2.35 mL | 4.7 mL |
| 10 mM | 0.24 mL | 1.18 mL | 2.35 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.47 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Muthumani et al (2004) Suppresssion of HIV-1 viral replication and cellular pathogenesis by a novel p38/JNK kinase inhibitor. AIDS 18 739 PMID: 15075508
See et al (2004) p38 mitogen activated protein kinase inhibition improves cardiac function and attenuates left ventricular remodeling fowllowing myocardial infarction in the rat. J.Am.Coll.Cardiol. 44 1679 PMID: 15489104
Wadsworth et al (1999) RWJ 67657, a potent, orally active inhibitor of p38 mitogen-activated protein kinase. J.Pharm.Exp.Ther. 291 680 PMID:
Keywords: RWJ 67657, supplier, Potent, selective, p38α, p38alpha, p38β, p38beta, inhibitors, inhibits, MAPK, Signaling, Signalling, Mitogen-Activated, Protein, Kinases, RWJ67657, p38, p38, Tocris Bioscience
