LY2886721 是选择性的，口服活性的 β 位淀粉样蛋白前体蛋白裂解酶 1 抑制剂，对重组人BACE1的IC50=20.3 nM。它对BACE1的选择性高于对组织蛋白酶 D、胃蛋白酶、肾素的选择性，但缺乏对BACE2的选择性。它可透过血脑屏障，并可用于研究阿尔茨海默氏病。

LY2886721, a BACE inhibitor, is used for the therapy of Alzheimer's Disease.

LY2886721 is an oral, small molecule of β-site amyloid protein cleaving enzyme (BACE) inhibitor with the potential to inhibit the synthesis of β-amyloid and thereby to slow the Clinicalal progression of AD. [1] LY2886721 can also targetγ-secretase to nhibit the synthesis of β-amyloid. [2]

The CTLs and NK cells (0.8×106/mL) are treated with the inhibitors L1 (10-20 μM) or Aloxistatin (20-30 μM) for 24 hr at 37°C in 24-well plates. Cells are then used in 51Cr-release assays or are lysed to examine perforin in Western blots. The inhibitor is also added at the same concentration during the 4 hr reactions in some 51Cr-release assays, as indicated. Cell lysates are prepared using NP-40 lysis buffer (25 mM HEPES, 250 mM NaCl, 2.5 mM ethylenediaminetetraacetic acid, 0.1% volume/volume Nonidet P-40) and total protein concentration is determined using the Bradford assay. Equal amounts of protein are loaded and resolved on 8% SDS-PAGE gels. Human or mouse perforin is detected using the appropriate antibodies as indicated. Anti-actin antibody is used as a loading control[2].

1262036-50-9

C18H16F2N4O2S

390.41

H2O:<1 mgml
Ethanol:<1 mgml
DMSO:9 mg/mL (23.05 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years