Biochem/physiol Actions

Target IC₅₀: 15 nM for BACE-1, human and 29 nM for sAPP_NF in HEK293-APP^NFEV cells

Reversible: yes

Primary Targetβ-Secretase

Cell permeable: yes

General description

A cell-permeable isophthalamide compound containing hydroxyethylamine motif that binds to BACE-1 active site and potently blocks its proteolytic activity (IC₅₀ = 15 nM for BACE-1, human and 29 nM for sAPP_NF in HEK293-APP^NFEV cells). Displays greater selectivity over other aspartyl proteases (IC₅₀ = 0.23 µM, 7.6 µM and >50 µM for BACE-2, cathepsin D, and renin, respectively). The solid form of this compound (Cat. No. 565788) is also available.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Stachel, S.J., et al. 2004. J. Med. Chem.47, 6447.

Packaging

500 µg in Glass bottle

Packaged under inert gas

Physical form

A 10 mM (500 µg/86.4 µL) solution of β-Secretase Inhibitor IV (Cat. No. 565788) in DMSO.

Reconstitution

Following initial thaw, aliquot and freeze (-70°C). Aliquots are stable for up to 6 months at -70°C. For short term storage, aliquots are stable for up to 3 months at -20°C.

Warning

Toxicity: Irritant (B)