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Sulindac sulfide

CAS No. : 49627-27-2

MCE 站：Sulindac sulfide

产品活性：Sulindac sulfide 是 γ-secretase 的一个非竞争性抑制剂，其对 γ₄₂-secretase 的 IC₅₀ 值为 20.2 μM。

研究领域：Neuronal Signaling  |  Stem Cell/Wnt

作用靶点：γ-secretase

In Vitro: Treatment with 100 μM of Sulindac sulfide (SSide) causes cell death presumably by inducing apoptosis, resulting in marked decrease in Aβgeneration as well as in total protein expression. The IC₅₀ value for Aβ42 secretion of Sulindac sulfide is 30.6±2.8 μM. SSone ａnd naproxen have no effect either on Aβ40 or Aβ42 secretion as well as on Notch cleavage up to 100 μM. It is observed that an inhibition of γ₄₂-secretase activity by Sulindac sulfide in a dose-dependent manner. The IC₅₀ value of SSide for inhibiting γ₄₂-secretase activity in vitro is 20.2±2.6 μM. A decrease is found in slope by the increase of the concentration of SSide in the plot of rate against the enzyme concentration, suggesting that Sulindac sulfide is not an irreversible or pseudo-irreversible inhibitor. Moreover, when the dialyzed solubilizedγ-secretase fraction is pretreated with Sulindac sulfide against CHAPSO buffer without Sulindac sulfide, γ-secretase activity is almost totally recovered. From these data, it is strongly suggested that the genuine molecular target of Sulindac sulfide is the γ-secretase complex ａnd that Sulindac sulfide works as a reversible γ-secretase inhibitor.

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