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Submit ReviewSB 239063
Description: Potent, selective p38 MAPK inhibitor; orally active
Chemical Name: trans-4-[4-(4-Fluorophenyl)-5-(2-methoxy-4-pyrimidinyl)-1H-imidazol-1-yl]cyclohexanol
Purity: ≥98% (HPLC)
Biological Activity for SB 239063
SB 239063 is a potent and selective p38 MAP kinase inhibitor (IC50 = 44 nM for p38α). Displays > 220-fold selectivity over ERK, JNK1 and other kinases; ~ 3-fold more selective than SB 203580 (Cat. Nos. 1202 and 1402). Reduces inflammatory cytokine production and is neuroprotective following oral administration in vivo.
Licensing Information
Sold for research purposes under agreement from GlaxoSmithKline
Technical Data for SB 239063
| M. Wt | 368.41 |
| Formula | C20H21FN4O2 |
| Storage | Desiccate at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 193551-21-2 |
| PubChem ID | 5166 |
| InChI Key | ZQUSFAUAYSEREK-UHFFFAOYSA-N |
| Smiles | O[C@@H]1CC[C@@H](N2C=NC(C4=CC=C(F)C=C4)=C2C3=CC=NC(OC)=N3)CC1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for SB 239063
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 3.68 | 10 with gentle warming |
Preparing Stock Solutions for SB 239063
The following data is based on the product molecular weight 368.41. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 27.14 mL | 135.72 mL | 271.44 mL |
| 0.5 mM | 5.43 mL | 27.14 mL | 54.29 mL |
| 1 mM | 2.71 mL | 13.57 mL | 27.14 mL |
| 5 mM | 0.54 mL | 2.71 mL | 5.43 mL |
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Product Datasheets for SB 239063
References for SB 239063
References are publications that support the biological activity of the product.
Barone et al (2001) SB 239063, a second-generation p38 mitogen-activated protein kinase inhibitor, reduces brain injury and neurological deficits in cerebral focal ischemia. J.Pharmacol.Exp.Ther. 296 312 PMID: 11160612
Legos et al (2002) The selective p38 inhibitor SB-239063 protects primary neurons from mild to moderate excitotoxic injury. Eur.J.Pharmacol. 447 37 PMID: 12106800
Underwood et al (2000) SB 239063, a potent p38 MAP kinase inhibitor, reduces inflammatory cytokine production, airways eosinophil infiltration, and persistence. J.Pharmacol.Exp.Ther. 293 281 PMID: 10734180
If you know of a relevant reference for SB 239063, please let us know.
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Keywords: SB 239063, SB 239063 supplier, Potent, selective, p38, MAP, kinases, inhibitors, inhibits, orally, active, MAPK, Signaling, Signalling, Mitogen-Activated, Protein, SB239063, GlaxoSmithKline, GSK, 1962, Tocris Bioscience
8 Citations for SB 239063
Citations are publications that use Tocris products. Selected citations for SB 239063 include:
Taoro-Gonzalez et al (2018) Hyperammonemia alters membrane expression of GluA1 and GluA2 subunits of AMPA receptors in hippocampus by enhancing activation of the IL-1 receptor: underlying mechanisms. J Neuroinflammation 15 36 PMID: 29422059
Potapova et al (2013) Caspases and p38 MAPK regulate endothelial cell adhesiveness for mesenchymal stem cells. Metab Brain Dis 8 e73929 PMID: 24069252
Agusti et al (2014) Rats with minimal hepatic encephalopathy due to portacaval shunt show differential increase of translocator protein (18 kDa) binding in different brain areas, which is not affected by chronic MAP-kinase p38 inhibition. J Mol Neurosci 29 955 PMID: 24307181
Yang et al (2015) Delayed activation of spinal microglia contributes to the maintenance of bone cancer pain in female Wistar rats via P2X7 receptor and IL-18. J Neurosci 35 7950 PMID: 25995479
He and Aizenman (2010) ERK signaling leads to mitochondrial dysfunction in extracellular zinc-induced neurotoxicity. J Neurochem 114 452 PMID: 20412391
Emery et al (2014) Separate cyclic AMP sensors for neuritogenesis, growth arrest, and survival of neuroendocrine cells. J Biol Chem 289 10126 PMID: 24567337
Ferreira et al (2011) Neuropeptide Y inhibits interleukin-1β-induced phagocytosis by microglial cells. PLoS One 8 169 PMID: 22136135
Dobreva et al (2006) Interleukin-8 secretion by fibroblasts induced by low density lipoproteins is p38 MAPK-dependent and leads to cell spreading and wound closure. J Biol Chem 281 199 PMID: 16251188
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Reviews for SB 239063
Average Rating: 5 (Based on 1 Review.)
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The role of p38 MAPK signaling in LPA induced pro-inflammatory phenotype in microglia cells.
By
Joanna Plastira on 06/08/2019
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: Primary murine microglia cells
The role of MAPK pathways (JNK, p38 and ERK) was studied in the LPA induced pro-inflammatory phenotype in microglia. In this case cells were incubated for the indicated time points with LPA (1µM) in the presence or absence of SB239063 (10µM) or SB203580 (10µM). A series of assays were performed. p38 MAPK inhibition totally decreased the expression of 4 pro-inflammatory transcription factors (here presented: pp65). Both inhibitors worked nicely and the results were consistent.
Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
MAPK Signaling Scientific Review
MAP kinase signaling is integral to the regulation of numerous cellular processes such as proliferation and differentiation, and as a result is an important focus of cancer and immunology research. Updated for 2016, this review discusses the regulation of the MAPK pathway and properties of MAPK cascades. Compounds available from Tocris are listed.
Pathways for SB 239063
