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Biological Data

Biological description Potent p38 MAPK inhibitor (IC50 values are 1.0 and 11 µM for p38α and β subunits respectively). Exhibits no activity at p38γ or δ subunits. Potently inhibits TNFα, IL-1β and IL-8 production (IC50 values are 15, 11 and 30 nM respectively). Also inhibits IL-6, IL-8, MMP3, COX-2 mRNA and HIV replication. Displays anti-inflammatory and cardioprotective properties. Approx 10-fold more potent than SB 203580.

Solubility & Handling

Storage instructions Room temperature
Solubility overview Soluble in DMSO (100mM) or ethanol (50mM)
Important This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.

Calculators

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Chemical Data

Purity >98%
Chemical name 4-[4-(4-Fluorophenyl)-1-(3-phenylpropyl)-5-(4-pyridinyl)-1H-imidazol-2-yl]-3-butyn-1-ol
Molecular Weight 425.5
Molecular Formula C27H24FN3O
CAS Number 215303-72-3
PubChem identifier 3008319
SMILES FC(C=C4)=CC=C4C(N=C(C#CCCO)N2CCCC3=CC=CC=C3)=C2C1=CC=NC=C1
InChiKey QSUSKMBNZQHHPA-UHFFFAOYSA-N

References for RWJ 67657

References are publications that support the biological activity of the product
  • Strong inhibition of TNF-alpha production and inhibition of IL-8 and COX-2 mRNA expression in monocyte-derived macrophages by RWJ 67657, a p38 mitogen-activated protein kinase (MAPK) inhibitor.

    Westra J et al (2004) Arthritis Res Ther 6(4) : R384-92.
  • p38 mitogen-activated protein kinase inhibition improves cardiac function and attenuates left ventricular remodeling following myocardial infarction in the rat.

    See F et al (2004) J Am Coll Cardiol 44(8) : 1679-89.
  • Suppression of HIV-1 viral replication and cellular pathogenesis by a novel p38/JNK kinase inhibitor.

    Muthumani K et al (2004) AIDS 18(5) : 739-48.
  • RWJ 67657, a potent, orally active inhibitor of p38 mitogen-activated protein kinase.

    Wadsworth SA et al (1999) J Pharmacol Exp Ther 291(2) : 680-7.

4 Item(s)