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Submit ReviewRWJ 67657 is a 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.
RWJ 67657 is also offered as part of the Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.
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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 42.55 | 100 | |
ethanol | 42.55 | 100 |
The following data is based on the product molecular weight 425.5. Batch specific molecular weights may vary from batch to batch due to the degree 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 |
References are publications that support the biological activity of the product.
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: 10525088
If you know of a relevant reference for RWJ 67657, please let us know.
Keywords: RWJ 67657, RWJ 67657 supplier, Potent, selective, p38α, p38alpha, p38β, p38beta, inhibitors, inhibits, MAPK, Signaling, Signalling, Mitogen-Activated, Protein, Kinases, RWJ67657, p38, 2999, Tocris Bioscience
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
MAP kinase signaling is integral to the regulation of numerous cellular processes such as proliferation and differentiation, and as a result is an important focus of cancer and immunology research. Updated for 2016, this review discusses the regulation of the MAPK pathway and properties of MAPK cascades. Compounds available from Tocris are listed.