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SB 239063

Catalog #: 1962
8 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
1962/10
SB 239063 | CAS No. 193551-21-2 | p38 Inhibitors
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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%

Product Details
Citations (8)
Reviews
Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

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.

Technical Data

M.Wt:
368.41
Formula:
C20H21FN4O2
Solubility:
Soluble to 10 mM in DMSO with gentle warming
Purity:
≥98%
Storage:
Desiccate at +4°C
CAS No:
193551-21-2

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.

Additional Information

Licensing Caveats:
Sold for research purposes under agreement from GlaxoSmithKline

Background References

  1. Sirt1, p53, and p38(MAPK) Are Crucial Regulators of Detrimental Phenotypes of Embryonic Stem Cells with Max Expression Ablation.
    Hishida T, Nozaki Y, Nakachi Y, Mizuno Y, Iseki H, Katano M, Kamon M, Hirasaki M, Nishimoto M, Okazaki Y, Okuda A
    Stem Cells, 2012;30(8):1634-44.
  2. Regulation of the CCL2 Gene in Pancreatic beta-Cells by IL-1beta and Glucocorticoids: Role of MKP-1.
    Burke S, Goff M, Updegraff B, Lu D, Brown P, Minkin S, Biggerstaff J, Zhao L, Karlstad M, Collier J
    PLoS ONE, 2012;7(10):e46986.
  3. Alamandine reduces leptin expression through the c-Src/p38 MAP kinase pathway in adipose tissue
    T Uchiyama, F Okajima, C Mogi, A Tobo, S Tomono, K Sato
    PLoS ONE, 2017;12(6):e0178769.
  4. SB 239063, a second-generation p38 mitogen-activated protein kinase inhibitor, reduces brain injury and neurological deficits in cerebral focal ischemia.
    Barone et al.
    J.Pharmacol.Exp.Ther., 2001;296:312
  5. The selective p38 inhibitor SB-239063 protects primary neurons from mild to moderate excitotoxic injury.
    Legos et al.
    Eur.J.Pharmacol., 2002;447:37
  6. SB 239063, a potent p38 MAP kinase inhibitor, reduces inflammatory cytokine production, airways eosinophil infiltration, and persistence.
    Underwood et al.
    J.Pharmacol.Exp.Ther., 2000;293:281

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Citations for SB 239063

The citations listed below are publications that use Tocris products. Selected citations for SB 239063 include:

8 Citations: Showing 1 - 8

  1. Hyperammonemia alters membrane expression of GluA1 and GluA2 subunits of AMPA receptors in hippocampus by enhancing activation of the IL-1 receptor: underlying mechanisms.
    Authors: Taoro-Gonzalez Et al.
    J Neuroinflammation  2018;15:36
  2. Delayed activation of spinal microglia contributes to the maintenance of bone cancer pain in female Wistar rats via P2X7 receptor and IL-18.
    Authors: Yang Et al.
    J Neurosci  2015;35:7950
  3. 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.
    Authors: Agusti Et al.
    J Mol Neurosci  2014;29:955
  4. Separate cyclic AMP sensors for neuritogenesis, growth arrest, and survival of neuroendocrine cells.
    Authors: Emery Et al.
    J Biol Chem  2014;289:10126
  5. Caspases and p38 MAPK regulate endothelial cell adhesiveness for mesenchymal stem cells.
    Authors: Potapova Et al.
    Metab Brain Dis  2013;8:e73929
  6. Neuropeptide Y inhibits interleukin-1β-induced phagocytosis by microglial cells.
    Authors: Ferreira Et al.
    PLoS One  2011;8:169
  7. ERK signaling leads to mitochondrial dysfunction in extracellular zinc-induced neurotoxicity.
    Authors: He and Aizenman
    J Neurochem  2010;114:452
  8. Interleukin-8 secretion by fibroblasts induced by low density lipoproteins is p38 MAPK-dependent and leads to cell spreading and wound closure.
    Authors: Dobreva Et al.
    J Biol Chem  2006;281:199

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