SB 239063

Pricing Availability Delivery Time Qty
Cat.No. 1962 - SB 239063 | C20H21FN4O2 | CAS No. 193551-21-2
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)
Datasheet
Citations (4)
Literature
Pathways

Biological Activity

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

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 3.68 10mM with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 368.41. Batch specific molecular weights may vary from batch to batch due to solvent 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
1 mM 2.71 mL 13.57 mL 27.14 mL
5 mM 0.54 mL 2.71 mL 5.43 mL
10 mM 0.27 mL 1.36 mL 2.71 mL
50 mM 0.05 mL 0.27 mL 0.54 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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


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Keywords: SB 239063, supplier, Potent, selective, p38, MAP, kinases, inhibitors, inhibits, orally, active, MAPK, Signaling, Signalling, Mitogen-Activated, Protein, SB239063, GlaxoSmithKline, GSK, p38, Tocris Bioscience

4 Citations for SB 239063

Citations are publications that use Tocris products. Selected citations for SB 239063 include:

Ferreira et al (2011) Neuropeptide Y inhibits interleukin-1β-induced phagocytosis by microglial cells. PLoS One 8 169 PMID: 22136135

He and Aizenman (2010) ERK signaling leads to mitochondrial dysfunction in extracellular zinc-induced neurotoxicity. J Neurochem 114 452 PMID: 20412391

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

Potapova et al (2013) Caspases and p38 MAPK regulate endothelial cell adhesiveness for mesenchymal stem cells. Metab Brain Dis 8 e73929 PMID: 24069252


Do you know of a great paper that uses SB 239063 from Tocris? If so please let us know.

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Reviews

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Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Immunology

Immunology Product Listing

A collection of over 190 products for immunology research, the guide includes research tools for the study of:

  • Chemokine and Cytokine Signaling
  • Chemotaxis
  • Complement System
  • Immune Cell Signaling
  • Inflammation
Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
MAPK Signaling

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

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.

Protocols

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