Dihydroergocristine mesylate (DHEC mesylate) 是γ-secretase (GSI) 的抑制剂, 可减少阿尔茨海默氏病淀粉样蛋白 β 肽 (amyloid-β) 的产生, 与 γ-secretase 和 Nicastrin 结合的平衡解离常数 (Kd) 值分别为 25.7 nM 和 9.8 μM。
Dihydroergocristine (DHEC) (2-20 μM; 24 hours) has an IC
50
value of 25 μM for inhibiting the activity of γ-secretase in T100 cells without affecting cell viability.
Dihydroergocristine (2-20 μM; 24 hours) inhibits cellular Aβ production and causes a dose-dependent accumulation of carboxy-terminal fragments of APP (APP-CTFs) in HEK293 and decreases γ-secretase activity in fibroblast cells.
Western Blot Analysis
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Cell Line:
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WT HEK293 cells; Fibroblast cells
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Concentration:
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2 μM, 5 μM, 10 μM, 20 μM
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Incubation Time:
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24 hours
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Result:
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Increased APP-CTFs accumulation in a dose-dependent manner.
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