Drug intelligence / Profile preview

CA-074Me

Development stage
Preclinical
Modality
Small Molecules
Administration
None Established; Used Primarily For Research Purposes (cell Culture/in Vitro/in Vivo Animal Studies)
01

Overview

CA-074Me is a cell-permeable small molecule inhibitor that selectively targets cathepsin B—a lysosomal cysteine protease involved in protein degradation and implicated in various pathological processes including cancer progression and neurodegeneration. As the methyl ester prodrug of CA‑074 (the active acid form), it is widely used as a research tool to study cathepsin B function in vitro and in vivo. It has not been approved for clinical use or advanced beyond preclinical/experimental stages. The compound acts by covalently binding to the active site of cathepsin B and inhibiting its proteolytic activity[1][6].

Other names
Methyl N-({(2S,3S)-3-[(propylamino)carbonyl]oxiran-2-yl}carbonyl)-L-isoleucyl-L-prolinatemethyl (2S)-1-[(2S,3S)-3-methyl-2-{[(2S,3S)-3-(propylcarbamoyl)oxiran-2-yl]formamido}pentanoyl]pyrrolidine-2-carboxylate[6]L-Proline N-[[(2S,3S)-3-(propylamino)carbonyl]-2-oxiranyl]carbonyl-L-isoleucyl-, methyl ester[1]Methyl N-{[(2S,3S)-3-(propylcarbamoyl)-2-oxiranyl]carbonyl}-L-isoleucyl-L-prolinate[1][6]
02

Targets

CTSB (Cathepsin B)CTSL (Cathepsin L)

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