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 / Product Datasheet / 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:
Li et al (2013) Flow-based pipeline for systematic modulation and analysis of 3D tumor microenvironments. PLoS One 13 1969. PMID: 23563587.
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.
View Related Products by Product Action
Keywords: GW 5074, supplier, Potent, selective, c-Raf1, kinases, inhibitors, inhibits, GW5074, Tocris Bioscience, Raf Kinase Inhibitor products
Find multiple products by catalog number
New Products in this Area
Potent and selective allosteric activator of AMPKPerifosine
PKB/Akt inhibitor; also modulates Kv2.1 currentRAF 265
Raf kinase and VEGFR-2 inhibitorCZC 25146
Potent LRRK2 inhibitorRo 3280
Potent and selective PLK1 inhibitorRMM 46
MSK/RSK family kinase inhibitorLTURM 34
Potent DNA-PK inhibitorMLi-2
Potent and selective LRRK2 inhibitorLTURM 36
PI 3-kinase δ inhibitorPI 3065
Potent and selective PI 3-kinase p110δ inhibitorAZ PFKFB3 67
Potent and selective PFKFB3 inhibitorSTOCK2S 26016
Lysine deficient protein kinase (WNK) signaling inhibitorrac-CCT 250863
Potent Nek2 inhibitorRoscovitine
Potent, selective cyclin-dependent kinase inhibitorEnzastaurin
Potent PKCβ inhibitorBMS 265246
Potent cdk1/2 inhibitorAutocamtide-2-related inhibitory peptide, myristoylated
CaM kinase II inhibitor; enhanced cell permeable derivative of Autocamtide-2-related inhibitory peptide
Follow Tocris on LinkedIn
Visit our LinkedIn page for the latest Tocris news, events and updates.