RWJ-67657 是一种可口服的选择性p38α和p38β抑制剂，IC50分别为 1 和 11 μM。它是心脏保护剂，具有抗炎和抗肿瘤活性。

RWJ-67657 is an orally active and selective p38α and p38β MAPK inhibitor (IC50s: 1 and 11 μM, respectively). RWJ-67657 shows no activity at p38γ and p38δ and shows a cardioprotective effect.

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 [2][3].

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 per day for 7 consecutive days) shows an effective anti-inflammatory effect. EPC transplantation plus RWJ-67657 administration synergistically promotes angiogenesis and neurogenesis after diabetic stroke by both improving the functioning of endothelial progenitor cells and reducing inflammation [2][4].

215303-72-3

C27H24FN3O

425.5

JNJ 3026582

DMSO:125 mg/mL (293.77 mM),ultrasonic and warming and heat to 60°C
Powder: -20°C for 3 years
In solvent: -80°C for 2 years