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Submit ReviewGW 5074
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)
Biological Activity for GW 5074
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.
Licensing Information
Sold for research purposes under agreement from Glaxo Wellcome Inc and Glaxo Group Ltd.
Technical Data for GW 5074
| 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 for GW 5074
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| ethanol | 1 | ||
| DMSO | 100 |
Preparing Stock Solutions for GW 5074
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.
| 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 for GW 5074
References for GW 5074
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
Xue et al (2023) Discovery of a drug-like, natural product-inspired DCAF11 ligand chemotype. Nat.Commun. 14 7908 PMID: 38036533
If you know of a relevant reference for GW 5074, please let us know.
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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
8 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
Meitzen et al (2011) β1-Adrenergic receptors activate two distinct signaling pathways in striatal neurons. J Neurochem 116 984 PMID: 21143600
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
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
Schaertl et al (2010) A profiling platform for the characterization of transglutaminase 2 (TG2) inhibitors. J Biomol Screen 15 478 PMID: 20395409
Kaiserman et al (2023) The Oxindole GW-5074 Inhibits JC Polyomavirus Infection and Spread by Antagonizing the MAPK-ERK Signaling Pathway mBio PMID: 36786589
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
Do you know of a great paper that uses GW 5074 from Tocris? Please let us know.
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