β-Secretase Inhibitor IV

A cell-permeable and potent inhibitor that binds to BACE-1 active site and 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 = 230 nM, 7.6 µM and >50 µM for BACE-2, cathepsin D, and renin, respectively).

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). Also available as a 10 mM solution in DMSO (Cat. No. 565794).

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Cell permeable: yes

Primary Target
BACE-1 human

Product does not compete with ATP.

Reversible: no

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

Packaged under inert gas

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Halima, S.B., et al. 2016. Cell Reports.14, In press.
Stachel, S.J., et al. 2004. J. Med. Chem.47, 6447.

Solubilize in DMSO (10 mg/ml), aliquot & store at -20*C; stable for 3 months.

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