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
Solubility overview
Soluble in DMSO (100mM) or ethanol (50mM)
Storage instructions
Room temperature
Storage of solutions
Prepare and use solutions on the same day if possible. Store solutions at -20°C for up to one month if storage is required. Equilibrate to RT and ensure the solution is precipitate free before use.
Shipping Conditions
Stable for ambient temperature shipping. Follow storage instructions on receipt.
Important
This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.
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.
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