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GW-5074

GW-5074 is an indole that functions as a highly selective Raf-1 (c-Raf) kinase inhibitor and is used to study Ras/Raf-1/ERK signaling. This compound inhibits desuccinylation activity of Sirt5 (a histone deacetylase), altering DNA repair and metabolism in vitro. GW-5074 is also neuroprotective against 6-OHDA toxicity, which is a commonly studied experimental model of Parkinson’s Disease.

References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/18929973

Cas No.

220904-83-6

Purity

≥98%

Formula

C15H8Br2INO2

Formula Wt.

520.94

Chemical Name

2H-Indol-2-one, 3-[(3,5-dibromo-4-hydroxyphenyl)methylene]-1,3-dihydro-5-iodo-

IUPAC Name

(3Z)-3-[(3,5-dibromo-4-hydroxyphenyl)methylidene]-5-iodo-1H-indol-2-one

Solubility

DMSO 104 mg/mL

Suenkel B, Fischer F, Steegborn C. Inhibition of the human deacylase Sirtuin 5 by the indole GW5074. Bioorg Med Chem Lett. 2013 Jan 1;23(1):143-6. PMID: 23195732.

Li J, Fan Y, Zhang YN, et al. The Raf-1 inhibitor GW5074 and the ERK1/2 pathway inhibitor U0126 ameliorate PC12 cells apoptosis induced by 6-hydroxydopamine. Pharmazie. 2012 Aug;67(8):718-24. PMID: 22957439.

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