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-APPNFEV 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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
β-Secretase
Reversible: yes
Target IC50: 15 nM for BACE-1, human and 29 nM for sAPP_NF in HEK293-APPNFEV cells
Packaging
Packaged under inert gas
Warning
Toxicity: Irritant (B)
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.
Other Notes
Stachel, S.J., et al. 2004. J. Med. Chem.47, 6447.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Shipping Information:
Dry Ice Surcharge & Ice Pack Shipments: $40
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- UPC:
- 51172431
- Condition:
- New
- Availability:
- 3-5 Days
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- MPN:
- 565794-500UG
- CAS:
- 797035-11-1
- Temperature Control Device:
- Yes
