GW5074 - 10mM in DMSO, high purity , CAS No.220904-83-6(DMSO)

Item Number
G408888
Grouped product items
SKUSizeAvailabilityPrice Qty
G408888-1ml
1ml
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$405.90

C-Raf/Raf-1 Selective Inhibitors

Basic Description

Specifications & PurityMoligand™, 10mM in DMSO
Biochemical and Physiological MechanismsGW5074 is a potent and selective c-Raf inhibitor with IC50 of 9 nM, no effect on the activities of JNK1/2/3, MEK1, MKK6/7, CDK1/2, c-Src, p38 MAP, VEGFR2 or c-Fms is noted. GW5074 inhibits LK-induced apoptosis.
Storage TempStore at -80°C
Shipped InIce chest + Ice pads
GradeMoligand™
Product Description

Information

GW5074 is a potent and selectivec-Rafinhibitor withIC50of 9 nM, no effect on the activities of JNK1/2/3, MEK1, MKK6/7, CDK1/2, c-Src, p38 MAP, VEGFR2 or c-Fms is noted. GW5074 inhibits LK-inducedapoptosis.
In vitro

GW5074 is a potent and specific inhibitor of c-Raf with IC50 of 9 nM and has no effect of MKK6, MKK7, p38 MAP kinase and cdks in vitro. However, treatment of neuronal cultures with GW5074 permits accumulation of activating modifications on c-Raf and also B-Raf. The inhibition of LK-induced apoptosis by GW5074 in cerebellar granule neurons is not MEK-ERK-dependent. GW5074 delays down-regulation of Akt activity but inhibits apoptosis by an Akt-independent mechanism. GW5074 affects Ras, nuclear factor-kappa B and c-jun. GW5074 inhibits cell death caused by neurotoxins in granule cells and other neuronal types.

In vivo

GW5074 is protective in an in vivo experimental model of Huntington’s disease. GW5074 (5 mg/Kg) completely prevented extensive bilateral striatal lesions induced by 3-NP in mice. GW5074 completely abolishes chronic morphine-mediated AC superactivation I in CHO cells stably expressing the humanμ-opioid receptor. GW5074 suppresses sidestream smoke-induced airway hyperresponsiveness in mice.
Cell Data

cell lines:

Concentrations:~5 μM

Incubation Time:24 hours

Powder Purity:≥99%

Associated Targets(Human)

CYP1A2 Tchem Cytochrome P450 1A2 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
RAF1 Tclin RAF proto-oncogene serine/threonine-protein kinase (4 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
BRAF Tclin Serine/threonine-protein kinase B-raf (9 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ARAF Tchem Serine/threonine-protein kinase A-Raf (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

Canonical SMILES OC1=C(Br)C=C(C=C1Br)C=C2C(=O)NC3=CC=C(I)C=C23
Molecular Weight 520.94

Certificates

Certificate of Analysis(COA)

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Chemical and Physical Properties

SolubilitySolubility (25°C) In vitro DMSO: 71 mg/mL (198.64 mM); Water: Insoluble; Ethanol: Insoluble;

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