An inhibitor of neutral sphingomyelinase (IC50 = 1 μM); selective for neutral sphingomyelinase over acid sphingomyelinase at concentrations up to 150 μM as well as B. cereus PC-PLC

GW 4869 (hydrochloride hydrate) – 10 mg

Brand:
Cayman
CAS:
6823-69-4
Storage:
-20
UN-No:
Non-Hazardous - /

Neutral sphingomyelinases mediate the release of ceramide from sphingomyelin in cellular membranes and can be activated by certain stresses. Ceramide can act as a signaling molecule in its own right, or it can be further processed to generate sphingosine (and sphingosine-1-phosphate). GW 4869 is an inhibitor of neutral sphingomyelinase (IC50 = 1 μM).{17163} It is selective for neutral sphingomyelinase over acid sphingomyelinase at concentrations up to 150 μM as well as B. cereus PC-PLC, human lyso-PAF PLC, and bovine PP2A at 10 μM. GW 4869 inhibits TNF-α-induced sphingomyelin hydrolysis by 100% when used at a concentration of 20 μM and TNF-α-induced cell death in MCF-7 cells.{17163,17164} It also reduces the inhibitory effects of oxidized 1-palmitoyl-2-arachidonyl-sn-glycero-3-phosphatidylcholine (OxPAPC) and the 5-keto-6-octendioic acid ester of 2-lysophosphatidylethanolamine (KOdiA-PE) on LPS-induction of IL-8 in human aortic endothelial cells.{17165} In vivo, GW 4869 (1 mg/kg) reverses hypoxia-induced pulmonary vasoconstriction in rats.{17166}  

 

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Description

An inhibitor of neutral sphingomyelinase (IC50 = 1 μM); selective for neutral sphingomyelinase over acid sphingomyelinase at concentrations up to 150 μM as well as B. cereus PC-PLC, human lyso-PAF PLC, and bovine PP2A at 10 μM; inhibits TNF-α-induced sphingomyelin hydrolysis and TNF-α-induced cell death in MCF-7 cells; reduces the inhibitory effects of OxPAPC and KOdiA-PE on LPS-induction of IL-8 in human aortic endothelial cells; reverses hypoxia-induced pulmonary vasoconstriction in rats at 1 mg/kg,

Formal name: 3,3′-(1,4-phenylene)bis[N-[4-(4,5-dihydro-1H-imidazol-2-yl)phenyl]-dihydrochloride-2-propenamide

Synonyms: 

Molecular weight: 577.5

CAS: 6823-69-4

Purity: ≥90%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Sphingolipid Turnover||Research Area|Immunology & Inflammation

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