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(S)-N-(4-carbamimidoylbenzyl)-1-(2-(cyclohexylamino)ethanoyl)pyrrolidine-2-carboxamide

Development stage
Unknown
Modality
Small Molecules
01

Overview

A synthetic small molecule inhibitor, (S)-N-(4-carbamimidoylbenzyl)-1-(2-(cyclohexylamino)ethanoyl)pyrrolidine-2-carboxamide is designed to target serine proteases, with a particular focus on hepsin. Hepsin is a type II transmembrane serine protease implicated in cancer progression and metastasis. This compound has demonstrated potent inhibitory activity against hepsin in biochemical assays, with reported Ki values in the low nanomolar range for specific stereoisomers. The molecule exhibits selectivity for hepsin over related proteases such as matriptase[5]. Its mechanism of action involves competitive inhibition at the active site of the enzyme, thereby blocking its proteolytic function.

Other names
(S)-N-(4-carbamimidoylbenzyl)-1-(2-(cyclohexylamino)ethanoyl)pyrrolidine-2-carboxamide
02

Targets

HPN (Hepsin)

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