GW 5074
Chemical Name: 3-(3,5-Dibromo-4-hydroxy-benzylidene)-5-iodo-1,3-dihydro-indol-2-one
Purity: ≥98%
Biological Activity
GW 5074 is a potent, selective and cell-permeable c-Raf1 kinase inhibitor (IC50 = 9 nM). GW 5074 displays ≥ 100-fold selectivity for raf kinase over CDK1, CDK2, c-src, ERK2, MEK, p38, Tie2, VEGFR2 and c-fm. GW 5074 binds mutant huntingtin (mHTT) and decreases levels of mHTT in cultured hippocampal neurons and fibroblasts from patients with Huntington's disease. Brain penetrant.Technical Data
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
Background References
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VEGF increases endothelial permeability by separate signaling pathways involving ERK-1/2 and nitric oxide.
Breslin et al.
Am.J.Physiol.Heart Circ.Physiol., 2003;284:H92 -
Inhibition of ATF-3 expression by B-Raf mediates the neuroprotective action of GW5074.
Chen et al.
J.Neurochem., 2008;105:1300 -
The discovery of potent cRaf1 kinase inhibitors.
Lackey et al.
Bioorg.Med.Chem.Lett., 2000;10:223 -
Involvement of Raf-1 in chronic delta-opioid receptor agonist-mediated adenylyl cyclase superactivation.
Varga et al.
Eur.J.Pharmacol., 2002;451:101 -
Allele-selective lowering of mutant HTT protein by HTT-LC3 linker compounds.
Li et al.
Nature, 2019;575:203
Product Datasheets
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Citations for GW 5074
The citations listed below are publications that use Tocris products. Selected citations for GW 5074 include:
8 Citations: Showing 1 - 8
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The Oxindole GW-5074 Inhibits JC Polyomavirus Infection and Spread by Antagonizing the MAPK-ERK Signaling Pathway
Authors: Kaiserman Et al.
mBio 2023;
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Flow-based pipeline for systematic modulation and analysis of 3D tumor microenvironments.
Authors: Li Et al.
PLoS One 2013;13:1969
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Pharmacological rescue of mitochondrial deficits in iPSC-derived neural cells from patients with familial Parkinson's disease.
Authors: Cooper Et al.
Sci Transl Med 2012;4:141ra90
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β1-Adrenergic receptors activate two distinct signaling pathways in striatal neurons.
Authors: Meitzen Et al.
J Neurochem 2011;116:984
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A profiling platform for the characterization of transglutaminase 2 (TG2) inhibitors.
Authors: Schaertl Et al.
J Biomol Screen 2010;15:478
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SimV. inhibits induction of matrix metalloproteinase-9 in rat alveolar macrophages exposed to cigarette smoke extract.
Authors: Kim Et al.
Exp Mol Med 2009;41:277
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Signaling of short- and long-term regulation of intestinal epithelial type 1 Na+/H+ exchanger by IF.-gamma.
Authors: Magro Et al.
Br J Pharmacol 2005;145:93
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Intestinal Na+-K+-ATPase activity and molecular events downstream of IF.-gamma receptor stimulation.
Authors: Magro Et al.
Br J Pharmacol 2004;142:1281
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