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Key Documents

G6416

Sigma-Aldrich

GW5074

powder

Synonym(s):

3-(3,5-Dibromo-4-hydroxybenzyliden)-5-iodo-1,3-dihydroindol-2-one

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About This Item

Empirical Formula (Hill Notation):
C15H8Br2INO2
CAS Number:
Molecular Weight:
520.94
MDL number:
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77

Assay

≥98% (HPLC)

Quality Level

form

powder

storage condition

protect from light

color

yellow to orange-brown

solubility

DMSO: 5 mg/mL, clear

storage temp.

room temp

SMILES string

Oc1c(Br)cc(cc1Br)\C=C2/C(=O)Nc3ccc(I)cc23

InChI

1S/C15H8Br2INO2/c16-11-4-7(5-12(17)14(11)20)3-10-9-6-8(18)1-2-13(9)19-15(10)21/h1-6,20H,(H,19,21)/b10-3-

InChI key

LMXYVLFTZRPNRV-KMKOMSMNSA-N

Gene Information

human ... RAF1(5894)

Application

GW5074 has been used as a specific inhibitor of cRaf1 in C2 murine skeletal myoblasts, HT-29 colorectal adenocarcinoma cell line and neutrophils.

Biochem/physiol Actions

GW5074 is a cRaf1 kinase inhibitor, which is placed immediately downstream of Ras in the Motogen activated protein kinase (MAPK) signaling pathway. It elicits protection in GW5074 prevents degeneration in Huntington′s disease and also have therapeutic potential in treating neurodegenerative disorders. GW5074 in combination with anti-inflammatory drug, dexamethasone, attenuates sidestream smoke-induced airway inflammation.

Other Notes

light sensitive

Legal Information

Sold for research purposes under agreement from Glaxo­Smith­Kline

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Personal Protective Equipment

dust mask type N95 (US), Eyeshields, Gloves

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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The c-Raf inhibitor GW5074 provides neuroprotection in vitro and in an animal model of neurodegeneration through a MEK-ERK and Akt-independent mechanism
Chin PC, et al.
Journal of Neurochemistry, 90(3), 595-608 (2004)
Human intestinal epithelial cells respond to beta-glucans via Dectin-1 and Syk
Cohen-Kedar S, et al.
European Journal of Immunology, 44(12), 3729-3740 (2014)
Yuan Zhang et al.
Scientific reports, 7(1), 10385-10385 (2017-09-06)
Enterovirus 71 (EV71) is a major pathogen of hand, foot, and mouth disease (HFMD). To date, no antiviral drug has been approved to treat EV71 infection. Due to the essential role that EV71 3 C protease (3C
Clement Opoku-Temeng et al.
Journal of proteomics, 202, 103368-103368 (2019-04-28)
Halogenated 4-hydroxybenzylidene indolinones have been shown to re-sensitize methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus faecalis (VRE) to methicillin and vancomycin respectively. The mechanism of antibiotic re-sensitization was however not previously studied. Here, we probe the scope of antibiotic re-sensitization
Tomoko Nishimura et al.
PloS one, 3(7), e2558-e2558 (2008-07-04)
Selective serotonin reuptake inhibitors (SSRIs) have been widely used and are a major therapeutic advance in psychopharmacology. However, their pharmacology is quite heterogeneous. The SSRI fluvoxamine, with sigma-1 receptor agonism, is shown to potentiate nerve-growth factor (NGF)-induced neurite outgrowth in

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