Biochem/physiol Actions

Cell permeable: no

Reversible: no

Primary Targethuman brain memapsin 2

Product does not compete with ATP.

Target K_i: 1.6 nM against recombinant memapsin 2; 9.58 nM against recombinant pro-memapsin 2; 48 nM against cathepsin D

General description

An eight residue peptidomimetic, tight binding transition-state analog inhibitor of human brain memapsin 2 (K_i = 1.6 nM, recombinant memapsin 2; K_i = 9.58 nM, recombinant pro-memapsin 2). Also inhibits cathepsin D (K_i = 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.

A peptidomimetic, highly potent, tight-binding transition-state analog inhibitor of human brain β-secretase (K_i = 1.6 nM, recombinant memapsin-2; K_i = 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 (K_i = 48 nM).

Legal Information

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

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.

Packaging

Packaged under inert gas

250 µg in Plastic ampoule

Physical form

A 1 mM (250µg in 280 µl) solution in DMSO. Supplied as a trifluoroacetate salt.

Reconstitution

Following initial thaw, aliquot and freeze (-20°C). Avoid freeze/thaw cycles of solutions.

Sequence

Glu-Val-Asn-Leu-Ψ-Ala-Ala-Glu-Phe [Ψ denotes replacement of CONH by (S)-CH(OH)CH₂]

Warning

Toxicity: Standard Handling (A)