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. 2009 Nov 19;285(3):1634–1642. doi: 10.1074/jbc.M109.066753

FIGURE 1.

FIGURE 1.

The β-cleavage of wild type and “Swedish mutant” APP substrates is inhibited with equal efficiency by BSIs in an in vitro BACE1 activity assay. A, SH-SY5Y cells stably transfected with wild type APP (APPwt; ■) or “Swedish mutant” APP (APPswe; ○) were treated with Inhibitor IV at the indicated concentrations for 24 h, and the conditioned medium was analyzed for the amount of Aβ1–40 as described under “Experimental Procedures.” Aβ1–40 quantification data are expressed relative to those for DMSO-treated control cultures (defined as 100%). The IC50 values for APPwt and APPswe are 61 and 694 nm, respectively. B, an in vitro BACE1 assay was performed using 0.45 nm purified human BACE1, 4 μm substrate peptide (a greater than 100-fold excess of substrate), and the indicated concentrations of BSI OM99–2 or Inhibitor IV. The inhibition data are expressed relative to control reaction mixtures lacking BACE1 enzyme (defined as 100%). However, 0% inhibition is defined as that obtained for a control solution treated with DMSO (no inhibitor).