product name SB239063
Description: SB239063 is a highly potent and selective p38 MAPKα/β inhibitor with IC50 of 44 nM, showing no activity against the γ- and δ-kinase isoforms. In lipopolysaccharide-stimulated human peripheral blood monocytes, SB 239063 inhibited interleukin-1 and tumor necrosis factor-alpha production (IC(50) values = 0.12 and 0.35 microM, respectively). SB 239063 may be useful for the treatment of asthma and other inflammatory disorders.
References: J Pharmacol Exp Ther. 2000 Apr;293(1):281-8; Eur J Pharmacol. 2008 Sep 11;592(1-3):55-61.
368.4
Formula
C20H21FN4O2
CAS No.
193551-21-2
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 60 mg/mL (162.9 mM)
Water: <1 mg/mL
Ethanol: 7 mg/mL warmed (19.0 mM)
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: SB 239063 potently inhibits IL-1 and TNF-α production in LPS-stimulated human peripheral blood monocytes with IC50 of 120 and 350 nM, respectively. In oxygen-glucose-deprived hippocampal slice cultures, SB239063 strikingly reduces the levels of the pro-inflammatory cytokine IL-1beta, causes cell death after oxygen-glucose deprivation and significantly diminishes microglia activation. In human corneal endothelial cell, SB 239063 inhibits TGF-β(2) and FGF-2-induced cell migration. Kinase Assay: SB 239063 is a potent and selective p38 MAPK inhibitor (IC50 = 44 nM for p38α). It displays > 220-fold selectivity over ERK, JNK1 and other kinases; and is ~ 3-fold more selective than SB 203580. Cell Assay: In oxygen-glucose-deprived hippocampal slice cultures, treatment with 20 μM and 100 μM SB239063 significantly reduced the levels of the pro-inflammatory cytokine IL-1β and reduced cell death after oxygen-glucose deprivation and strikingly diminished microglia activation. |
|---|---|
| In Vivo | In both guinea pigs and mice, SB 239063 (10 mg/kg, p.o.) reduces antigen-induced airway eosinophilia. In air- and ozone-exposed C57/BL6 and MKP-1(-/-) mice, SB239063 inhibits bronchial contraction. |
| Animal model | Guinea pigs |
| Formulation & Dosage | Dissolved in acidified 0.5% Tragacanth; 30 mg/kg; p.o. |
| References | J Pharmacol Exp Ther. 2000 Apr;293(1):281-8; Eur J Pharmacol. 2008 Sep 11;592(1-3):55-61. |
