Cayman E2012

E2012 is a modulator of γ-secretase.¹ It selectively inhibits APP intracellular signaling domain (AICD) cleavage to amyloid-β (Aβ) over Notch cleavage to its signaling effector Notch intracellular domain (NICD), processes both mediated by γ-secretase, when used at a concentration of 1 µM in luciferase assays.² E2012 also inhibits the activity of the cholesterol synthesis enzyme 3β-hydroxysterol ∆²⁴-reductase (DHCR24) in primary rat hepatocytes and HepG2 cells (IC₅₀s = 11 and 15 nM, respectively).³ It reduces Aβ (1-42) (Aβ42) production in primary rat embryonic cerebral cortex neurons with an IC₅₀ value of 220 nM.⁴ E2012 (100 mg/kg) also decreases Aβ42 levels in guinea pig brain and cerebral spinal fluid (CSF).⁴

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