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)
Reviews
Literature (3)

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. Also binds mutant huntingtin (mHTT). Decreases levels of mHTT in cultured hippocampal neurons and fibroblasts from patients with Huntington's disease.

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 OC(C(Br)=C1)=C(Br)C=C1/C=C(C2=CC(I)=CC=C2N3)\C3=O

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
ethanol 1
DMSO 100

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 the degree 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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References

References are publications that support the biological activity of the product.

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

Li et al (2019) Allele-selective lowering of mutant HTT protein by HTT-LC3 linker compounds. Nature 575 203 PMID: 31666698


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Keywords: GW 5074, GW 5074 supplier, Potent, selective, c-Raf1, kinases, inhibitors, inhibits, GW5074, mHTT, huntingtin, huntingtons, disease, Raf, Kinase, 1381, Tocris Bioscience

7 Citations for GW 5074

Citations are publications that use Tocris products. Selected citations for GW 5074 include:

Schaertl et al (2010) A profiling platform for the characterization of transglutaminase 2 (TG2) inhibitors. J Biomol Screen 15 478 PMID: 20395409

Magro et al (2005) Signaling of short- and long-term regulation of intestinal epithelial type 1 Na+/H+ exchanger by IF.-gamma. Br J Pharmacol 145 93 PMID: 15723092

Magro et al (2004) Intestinal Na+-K+-ATPase activity and molecular events downstream of IF.-gamma receptor stimulation. Br J Pharmacol 142 1281 PMID: 15277314

Kim et al (2009) SimV. inhibits induction of matrix metalloproteinase-9 in rat alveolar macrophages exposed to cigarette smoke extract. Exp Mol Med 41 277 PMID: 19299917


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Literature in this Area

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