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Category: EnzymesarrowKinasesarrowcRaf Kinase
Cat.No. Product Name
1381 GW 5074
Price and Availability

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GW 5074

Other Information:

Sold for research purposes under agreement from Glaxo Wellcome Inc and Glaxo Group Ltd
Chemical Name: 3-(3,5-Dibromo-4-hydroxy-benzylidene)-5-iodo-1,3-dihydr o-indol-2-one

Biological Activity:

Potent, selective and cell-permeable cRaf1 kinase inhibitor (IC50 = 9 nM). Displays ³ 100-fold selectivity for raf kinase over CDK1, CDK2, c-src, ERK2, MEK, p38, Tie2, VEGFR2 and c-fm.

Technical Data:

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M.Wt: 520.94
Formula: C15H8Br2INO2
Storage: Desiccate at -20°C
Solubility: Soluble to 1 mM in Ethanol and to 100 mM in DMSO
Purity: >98%
CAS No: [220904-83-6]

Resources:

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    • Certificate of Analysis / MSDS:

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    References:

    Lackey et al (2000) The discovery of potent cRaf1 kinase inhibitors. Bioorg.Med.Chem.Lett. 10 223. Varga et al (2002) Involvement of Raf-1 in chronic delta-opioid receptor agonist-mediated adenylyl cyclase superactivation. Eur.J.Pharmacol. 451 101. 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.
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    Keywords: GW 5074, Kinases, Potent, Selective CRaf1 Kinase Inhibitor, GW5074, Tocris Bioscience
    Literature in this Area
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    Signal Transduction Guide : An informative guide for all scientists working in: Cell cycle & apoptosis, Protein kinases & phosphatases, Ion channels, Calcium & lipid signaling, Cyclic nucleotides & G-proteins, Nitric oxide, & Signaling EnzymesA complete listing of signal transduction products available from Tocris, including descriptions on selected tools and unit sizes.
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