GW 5074

Name: GW 5074
Brand: Tocris Bioscience
SKU: 1381

Tocris Bioscience, part of Bio-Techne | Catalog # 1381

Citations (35)

COA / SDS

Potent, selective c-Raf1 kinase inhibitor

Key Product Details

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)
Molecular Weight:	520.94

View Full Technical Details for GW 5074

Technical Data
Citations

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 for GW 5074

	Solvent	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	9.60 mL	19.20 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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References for GW 5074

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

Xue Discovery of a drug-like, natural product-inspired DCAF11 ligand chemotype. Nat.Commun. 2023 PMID: 38036533
Li Allele-selective lowering of mutant HTT protein by HTT-LC3 linker compounds. Nature 2019 PMID: 31666698
Varga Involvement of Raf-1 in chronic delta-opioid receptor agonist-mediated adenylyl cyclase superactivation. Eur.J.Pharmacol. 2002 PMID: 12223234
Lackey The discovery of potent cRaf1 kinase inhibitors. Bioorg.Med.Chem.Lett. 2000 PMID: 10698440
Chen Inhibition of ATF-3 expression by B-Raf mediates the neuroprotective action of GW5074. J.Neurochem. 2008 PMID: 18194435
Breslin VEGF increases endothelial permeability by separate signaling pathways involving ERK-1/2 and nitric oxide. Am.J.Physiol.Heart Circ.Physiol. 2003 PMID: 12388327