GW 5074

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Cat.No. 1381 - GW 5074 | C15H8Br2INO2 | CAS No. 220904-83-6
Description: Potent, selective c-Raf1 kinase inhibitor
Chemical Name: 3-(3,5-Dibromo-4-hydroxy-benzylidene)-5-iodo-1,3-dihydro-indol-2-one
Purity: ≥98% (HPLC)
Datasheet
Citations (7)
Literature

Biological Activity

Potent, 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 Information

Sold for research purposes under agreement from Glaxo Wellcome Inc and Glaxo Group Ltd.

Technical Data

M. Wt 520.94
Formula C15H8Br2INO2
Storage Desiccate at -20°C
Purity ≥98% (HPLC)
CAS Number 220904-83-6
PubChem ID 5924208
InChI Key LMXYVLFTZRPNRV-KMKOMSMNSA-N
Smiles OC1=C(Br)C=C(\C=C2/C(=O)NC3=CC=C(I)C=C23)C=C1Br

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.

Solubility Data

SolubilitySoluble to 1 mM in ethanol and to 100 mM in DMSO

Preparing Stock Solutions

The following data is based on the product molecular weight 520.94. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.92 mL 9.6 mL 19.2 mL
5 mM 0.38 mL 1.92 mL 3.84 mL
10 mM 0.19 mL 0.96 mL 1.92 mL
50 mM 0.04 mL 0.19 mL 0.38 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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

Chen et al (2008) Inhibition of ATF-3 expression by B-Raf mediates the neuroprotective action of GW5074. J.Neurochem. 105 1300 PMID: 18194435

Lackey et al (2000) The discovery of potent cRaf1 kinase inhibitors. Bioorg.Med.Chem.Lett. 10 223 PMID: 10698440

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


If you know of a relevant reference for GW 5074, please let us know.

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Keywords: Potent selective c-Raf1 kinases inhibitors inhibits GW5074 Raf Kinase

7 Citations for GW 5074

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


Do you know of a great paper that uses GW 5074 from Tocris? If so please let us know.

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A collection of over 400 products for kinase research, the listing includes inhibitors of:

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Pathways for GW 5074

Protocols

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