567715
N-SMase Inhibitor, GW4869
Sphingomyelinase, Neutral, Inhibitor GW4869, GW69A, GW554869A
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Merck KGaA
Frankfurter Str. 250
64293 Darmstadt
Germany
Phone: +49 6151 72-0
Fax: +49 6151 72 2000
01 June 2012
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A cell-permeable, symmetrical dihydroimidazolo-amide compound that acts as a potent, specific, non-competitive inhibitor of N-SMase (neutral sphingomyelinase) [IC50 = ~ 1 µM, rat brain; Km for sphingomyelin ~13 µM]. Does not inhibit human A-SMase (acid sphingomyelinase) even at 150 µM. Weakly inhibits the activities of bovine protein phosphatase 2A and mammalian lyso-PAF PLC, while no inhibition is observed for bacterial phosphatidylcholine-specific PLC. Reported to offer complete protection against TNF-α or diamine-induced cell death in MCF7 breast cancer cells at 20 µM. Does not modify the intracellular glutathione levels or interfere with TNF-α or diamine-mediated signaling effects.
| Product information | |||
|---|---|---|---|
| Form | Pale yellow solid | ||
| Primary Target | N-Smase rat brain | ||
| Primary Target IC50 | 1 µM | ||
| Molar mass | 577.5 | ||
| Protect from Light | Yes | ||
| Hygrocopic | Yes | ||
| Packaged under inert gas | Yes | ||
| Cell permeable | Yes | ||
| Purity | ≥90% by HPLC | ||
| Solubility | DMSO | ||
| Chemical formula | C30H28N6O2 • 2HCl | ||
| CAS number | 6823-69-4 | ||
| Store and ship information | |||
|---|---|---|---|
| Storage | -20°C | ||
| Ship |
Blue Ice Only
Standard Handling |
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