SB 239063

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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)
Citations (8)
Reviews (1)
Literature (1)
Pathways (1)

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
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
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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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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

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

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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.

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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

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

MAPK Signaling Pathway

MAPK Signaling Pathway

The mitogen-activated protein kinase pathway evokes an intracellular signaling cascade in response to extracellular stimuli such as heat and stress. It can influence cell division, metabolism and survival.