SB 239063

SKU: orb1225803

Description

A potent, selective, orally available p38 MAPK inhibitor with IC50 of 44 nM for both p38α and p38β; shows no activity (>100 μM) against the γ- and δ-kinase isoforms, and a panel of protein kinase; inhibits IL-1 and TNF-alpha production in LPS-stimulated human PBMCs (IC50= 0.12 and 0.35 uM); reduces inflammatory cytokine production, airways eosinophil infiltration and persistence in vivo.

Key Properties

• CAS Number: 193551-21-2
• MW: 368.4048
• Purity: >98% (HPLC)
• Formula: C₂₀H₂₁FN₄O₂
• SMILES: O[C@H]1CC[C@H](N2C(C3=NC(OC)=NC=C3)=C(C4=CC=C(F)C=C4)N=C2)CC1
• Target: p38 MAPK
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  Animal model: Male BALB/c mice (18–20 g). Dosage: 12 mg/kg. Administration: Oral administration; 1 h before and 4 h after OA challenge; bis in die for 3 days. Result: Significantly inhibited the resultant antigen-induced airway eosinophilia.
• In Vitro:
  Apoptosis Analysis Cell line: Eosinophils (guinea pig BALs). Concentration: 0.1 μM, 1 μM, 10 μM Incubation time: 29 hours, 47 hours. Result: Increased apoptosis of eosinophils in a dose-related in the presence of 10 pM IL-5 at every time point from 21 hours onwards.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SB-239063 | SB239063

Quick Database Links

Gene Symbol

p38 MAPK