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D609 is a xanthate and a competitive inhibitor of phosphatidylcholine-specific phospholipase C (PC-PLC; Ki = 6.4 μM). It has no effect on bacterial phosphatidylinositol-specific PLC, bovine pancreatic PLA2, or phospholipase D. D609 reduces sphingomyelin synthase activity by 55.5 and 90.5% in membrane preparations when used at concentrations of 100 and 200 mg/ml, respectively. Similar to other xanthates, D609 has antioxidant, antiviral, and anti-tumor activities. In addition, it has anti-inflammatory actions, inhibiting LPS-stimulated expression of nitric oxide synthase (NOS) in phagocytes (IC50 = 20 μg/ml) and IL-1β-induced expression of vascular cell adhesion molecule 1 (VCAM-1) in endothelial cells.
Chemische Eigenschaften
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Verwenden
D609 has been used as a phosphatidylcholine-specific phospholipase C (PC-PLC) inhibitor in mouse bone marrow derived monocytes. D609 has also been reported to significantly reduce the elevated levels of phosphatidylethanolamine binding protein 1 (PEBP1) in apolipoprotein E-/- mice.
Biologische Aktivit?t
Selective competitive phosphatidyl choline-specific phospholipase C (PC-PLC) inhibitor (K i = 6.4 μ M); antiviral and antitumor agent. Suppresses LPS- and IFN γ -induced NO production (IC 50 = 20 mg/ml) and blocks oxidative glutamate toxicity in nerve cells. Antioxidant in vivo .