Merck, 496000-250UG, OM99-2

General description
A peptidomimetic, highly potent, tight-binding transition-state analog inhibitor of human brain β-secretase (Ki = 1.6 nM, recombinant memapsin-2; Ki = 9.58 nM, recombinant pro-memapsin 2). Designed from the template of the β-secretase site of Swedish β-amyloid precursor protein (APP) with Asp to Ala replacement. Includes a nonhydrolyzable hydroxyethylene isostere between Leu and Ala. Also reported to inhibit cathepsin D at higher levels (Ki = 48 nM).
An eight residue peptidomimetic, tight binding transition-state analog inhibitor of human brain memapsin 2 (Ki = 1.6 nM, recombinant memapsin 2; Ki = 9.58 nM, recombinant pro-memapsin 2). Also inhibits cathepsin D (Ki = 48 nM). This aspartyl protease inhibitor is designed from the template of the β-secretase site of Swedish β-amyloid precursor protein (APP) with Asp to Ala replacement; also includes a nonhydrolyzable hydroxyethylene isostere between Leu and Ala.
Biochem/physiol Actions
Cell permeable: no
Primary Target
human brain memapsin 2
Product does not compete with ATP.
Reversible: no
Target Ki: 1.6 nM against recombinant memapsin 2; 9.58 nM against recombinant pro-memapsin 2; 48 nM against cathepsin D
Packaging
Packaged under inert gas
Physical form
A 1 mM (250µg in 280 µl) solution in DMSO. Supplied as a trifluoroacetate salt.
Preparation Note
Following initial thaw, aliquot and freeze (-20°C). Avoid freeze/thaw cycles of solutions.
Other Notes
Ghosh, A.K., et al. 2001. J. Med. Chem.44, 2865.
Turner III, R.T., et al. 2001. Biochemistry40, 10001.
Ghosh, A.K., et al. 2000. J. Am. Chem. Soc.122, 3522.
Hong, L., et al. 2000. Science290,150.
Glu-Val-Asn-Leu-Ψ-Ala-Ala-Glu-Phe [Ψ denotes replacement of CONH by (S)-CH(OH)CH₂]
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)