Cat. No. 1381
Chemical Name: 3-(3,5-Dibromo-4-hydroxy-benzyliden
Biological ActivityPotent, selective and cell-permeable c-Raf1 kinase inhibitor (IC50 = 9 nM). Displays ≥ 100-fold selectivity for raf kinase over CDK1, CDK2, c-src, ERK2, MEK, p38, Tie2, VEGFR2 and c-fm.
Licensing InformationSold for research purposes under agreement from Glaxo Wellcome Inc and Glaxo Group Ltd.
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.
Certificate of Analysis / Safety Data Sheet
Chen et al (2008) Inhibition of ATF-3 expression by B-Raf mediates the neuroprotective action of GW5074. J.Neurochem. 105 1300. PMID: 18194435.
Breslin et al (2003) VEGF increases endothelial permeability by separate signaling pathways involving ERK-1/2 and nitric oxide. Am.J.Physiol.Heart Circ.Physiol. 284 H92. PMID: 12388327.
Varga et al (2002) Involvement of Raf-1 in chronic delta-opioid receptor agonist-mediated adenylyl cyclase superactivation. Eur.J.Pharmacol. 451 101. PMID: 12223234.
Lackey et al (2000) The discovery of potent cRaf1 kinase inhibitors. Bioorg.Med.Chem.Lett. 10 223. PMID: 10698440.
If you know of a relevant reference for this product please let us know.
Citations are publications that use Tocris products. Selected citations for GW 5074 include:
Cooper et al (2012) Pharmacological rescue of mitochondrial deficits in iPSC-derived neural cells from patients with familial Parkinson's disease. Sci Transl Med 4 141ra90. PMID: 22764206.
Meitzen et al (2011) β1-Adrenergic receptors activate two distinct signaling pathways in striatal neurons. J Neurochem 116 984. PMID: 21143600.
Schaertl et al (2010) A profiling platform for the characterization of transglutaminase 2 (TG2) inhibitors. J Biomol Screen 15 478. PMID: 20395409.
Kim et al (2009) Simvastatin inhibits induction of matrix metalloproteinase-9 in rat alveolar macrophages exposed to cigarette smoke extract. Exp Mol Med 41 277. PMID: 19299917.
Magro et al (2005) Signaling of short- and long-term regulation of intestinal epithelial type 1 Na+/H+ exchanger by interferon-gamma. Br J Pharmacol 145 93. PMID: 15723092.
Magro et al (2004) Intestinal Na+-K+-ATPase activity and molecular events downstream of interferon-gamma receptor stimulation. Br J Pharmacol 142 1281. PMID: 15277314.
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Keywords: GW 5074, supplier, Potent, selective, c-Raf1, kinases, inhibitors, inhibits, GW5074, Tocris Bioscience, Raf Kinase Inhibitor products
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