Chemical Name: 3-(3,5-Dibromo-4-hydroxy-benzylidene)-5-iodo-1,3-dihydro-indol-2-one
Biological ActivityGW 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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
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.
The discovery of potent cRaf1 kinase inhibitors.
Lackey et al.
Involvement of Raf-1 in chronic delta-opioid receptor agonist-mediated adenylyl cyclase superactivation.
Varga et al.
Allele-selective lowering of mutant HTT protein by HTT-LC3 linker compounds.
Li et al.
Citations for GW 5074
The citations listed below are publications that use Tocris products. Selected citations for GW 5074 include:
7 Citations: Showing 1 - 7
Flow-based pipeline for systematic modulation and analysis of 3D tumor microenvironments.
Authors: Li Et al.
PLoS One 2013;13:1969
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
β1-Adrenergic receptors activate two distinct signaling pathways in striatal neurons.
Authors: Meitzen Et al.
J Neurochem 2011;116:984
A profiling platform for the characterization of transglutaminase 2 (TG2) inhibitors.
Authors: Schaertl Et al.
J Biomol Screen 2010;15:478
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
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
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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