RWJ-67657

SKU: orb1307766

Description

RWJ-67657 is a selective, orally bioavailable inhibitor of p38α and p38β MAP kinases with IC50 values of 1 μM and 11 μM, respectively. It exhibits cardioprotective properties and is utilized in research exploring inflammation, cardiovascular disease, and cellular stress responses in both in vitro and in vivo models.

Research Area

Signal Transduction

Key Properties

• CAS Number: 215303-72-3
• MW: 425.5
• Purity: 99.66% (May vary between batches)
• Formula: C₂₇H₂₄FN₃O
• SMILES: OCCC#Cc1nc(c(-c2ccncc2)n1CCCc1ccccc1)-c1ccc(F)cc1
• Target: p38 MAPK
• Solubility: DMSO:125 mg/mL (293.77 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (9.4 mM)

Bioactivity

• Target IC50:
  p38β:11 μM|p38α:1 μM
• In Vivo:
  RWJ-67657 inhibits TNF-alpha production in lipopolysaccharide-injected mice (87% inhibition at 50 mg/kg) and in rats (91% inhibition at 25 mg/kg) after oral administration. RWJ-67657 (50 mg/kg; p.o.; once daily for 7 consecutive days) demonstrates effective anti-inflammatory activity. EPC transplantation combined with RWJ-67657 administration synergistically promotes angiogenesis and neurogenesis following diabetic stroke by enhancing endothelial progenitor cell function and reducing inflammation .
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• In Vitro:
  RWJ-67657 suppresses the release of TNF-α by lipopolysaccharide (LPS)-treated human peripheral blood mononuclear cells (IC50: 3 nM) and the release of TNF-α from peripheral blood mononuclear cells treated with the superantigen staphylococcal enterotoxin B (IC50: 13 nM). RWJ67657 (10 μM; 24 hours) reduces colony formation in MCF-7 cells .
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

cardio, anti-tumor, Inhibitor, MCF-7, inhibit, JNJ3026582, JNJ-3026582, JNJ 3026582, inflammation, RWJ 67657, RWJ67657, RWJ-67657, protective. Anti-inflammatory, p38α, p38β, p38MAPK, p38 MAPK

Compound Identifiers

PubChem CID

3008319