GW554869A
GW69A
Sphingomyelinase, Neutral, Inhibitor GW4869 Pale yellow solid. PROTECT FROM LIGHT. HYGROSCOPIC. PACKAGED UNDER INERT GAS. 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-a or diamine-induced cell death in MCF7 breast cancer cells at 20 µM. Does not modify the intracellular glutathione levels or interfere with TNF-a or diamine-mediated signaling effects. Purity: ≥90% by HPLC. CAS 6823-69-4. Ref.: Marchesini, N., et al. 2003. J. Biol. Chem. In press. Luberto, C., et al. 2002. J. Biol. Chem. 277, 41128 Okamoto, Y., et al. 2002. FEBS Lett. 530, 140.
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