SB 239063

SB 239063 is a potent, selective and orally active p38 MAPK inhibitor, exhibits an IC₅₀ of 44 nM for recombinant purified human p38α, with equipotent inhibitory activity against p38α and p38β. SB 239063 has no effect on p38γ or p38δ. With anti-asthma activity and also be used to enhance memory which is impaired due to aging or medical conditions, such as, AD. SB 239063 can penetrate the blood brain barrier (BBB)^[1][2][3]. IC50 & Target:IC50: 44 nM (Human p38α)^[1] In Vitro:SB 239063 (0.1–10 μM ; 29 hours, 47 hours) increases apoptosis of eosinophils in a dose-related in the presence of 10 pM IL-5 at every time point from 21 hours onwards^[1].
SB 239063 potently inhibits IL-1 and TNF- a production in LPS-stimulated human peripheral blood monocytes with IC₅₀ values of 120 nM and 350 nM, respectively^[1].
In Vivo:SB 239063 (12 mg/kg; p.o.; 1 hour before and 4 hours after OA challenge; b.i.d. for 3 days) significantly inhibits the resultant antigen-induced airway eosinophilia^[1].
SB 239063 (12 mg/kg; p.o.) almost abolishes ovalbumin (OA)-induced airway eosinophilia (~ 93% inhibition) by inhalation^[1].
SB 239063 is a potent inhibitor of LPS-induced TNF-alpha production in the mouse peritoneal cavity with an EC₅₀ of 5.8 mg/kg (2.8–10.3; 95% CL)^[1].