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    SB239063
    SB239063

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0483
    CAS #: 193551-21-2Purity ≥98%

    Description: SB239063 (SB-239063) is a novel, highly potent, orally bioactive and selective p38 MAPKα/β inhibitor with potential anti-inflammatory activity. It inhibits p38 MAPKα/β with an IC50 of 44 nM, and shows no/little activity against the p38 MAPK γ- and δ-isoforms. SB 239063 displays > 220-fold selectivity for p38 MAPK over ERK, JNK1 and other kinases; and is around 3-fold more selective than SB 203580. In LPS (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.

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    Molecular Weight (MW)368.4
    FormulaC20H21FN4O2
    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)
    Other infoChemical Name: (1r,4r)-4-(4-(4-fluorophenyl)-5-(2-methoxypyrimidin-4-yl)-1H-imidazol-1-yl)cyclohexanol
    InChi Key: ZQUSFAUAYSEREK-WKILWMFISA-N
    InChi Code: InChI=1S/C20H21FN4O2/c1-27-20-22-11-10-17(24-20)19-18(13-2-4-14(21)5-3-13)23-12-25(19)15-6-8-16(26)9-7-15/h2-5,10-12,15-16,26H,6-9H2,1H3/t15-,16-
    SMILES Code: O[[email protected]]1CC[[email protected]](N2C(C3=NC(OC)=NC=C3)=C(C4=CC=C(F)C=C4)N=C2)CC1
    SynonymsSB 239063; SB-239063; SB239063


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    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 VivoIn 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 modelGuinea pigs
    Formulation & DosageDissolved 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.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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