Small-molecule inhibitor: AK295

Summary Literature

Name

Common name
AK295
Other names
calpain inhibitor XI; CX295

Inhibition

Peptidases inhibited
Compound AK295 was developed (Bartus et al., 1994) from a series of peptide alpha-ketoamide inhibitors described by Li et al.. (1993). It has Ki 27 - 42 nM for calpain 1 and calpain 2, but much weaker inhibition of cathepsin B (Saatman et al., 1996).
Mechanism
Inhibition is reversible.

Chemistry

CID at PubChem
183798
Structure
[AK295 (C02.001, C02.002 inhibitor) structure ]
Chemical/biochemical name
Z-Leu-aminobutyric acid-CONH(CH2)3-morpholine
Formula weight
505