β-Secretase Inhibitor IV, a cell-permeable isophthalamide compound containing a hydroxyethylamine motif which binds to BACE-1 active site and potently blocks its proteolytic activity. The compound displays greater selectivity over other aspartyl proteases. β-Secretase Inhibitor IV is an inhibitor of BACE and BACE2.
Stachel, S.J., et al. 2004. J. Med. Chem. 47, 6447.
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
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JiaranaikulwanitchJiaranaikulwanitch, J. et al. (PubMed 22781443) modified the tryptoline and tryptamine cores of BACE1 inhibitors previously identified by virtual screening in silico for additional modes of action. These core structures were readily linked to different side chains using 1,2,3-triazole rings as bridges by copper catalyzed azide-alkyne cycloaddition reactions. The neuroprotective effects of the multifunctional compounds 6h, 12c and 12h on A induced neuronal cell death at 1 M were significantly greater than those of the potent single target compound, BACE1 inhibitor IV and were comparable to curcumin. -SCBT Publication Review
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