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methyl (1R,2S)-2-(hydroxycarbamoyl)-1-{4-[(2-methylquinolin-4-yl)methoxy]benzyl}cyclopropanecarboxylate

Development stage
Preclinical
Lead developer
Merck
Modality
Small Molecules
01

Overview

This compound is a synthetic small molecule belonging to the class of quinoline derivatives. It is a cyclopropane-based hydroxamic acid designed as a potent and selective inhibitor of tumor necrosis factor-alpha converting enzyme (TACE), also known as ADAM17. TACE is involved in the proteolytic cleavage of membrane-bound TNF-alpha to its soluble form and plays a key role in inflammatory processes and certain cancers. This compound has demonstrated picomolar affinity for TACE with good selectivity over related metalloproteinases such as MMPs and ADAM10 in preclinical studies. It was developed primarily for research purposes and has not advanced to clinical development or approval[5][6].

Other names
methyl (1R,2S)-2-(hydroxycarbamoyl)-1-{4-[(2-methylquinolin-4-yl)methoxy]benzyl}cyclopropanecarboxylatemethyl (1R,2S)-2-(hydroxycarbamoyl)-1-{4-[(2-methylquinolin-4-yl)methoxy]phenyl}methyl)cyclopropane-1-carboxylateCyclopropanecarboxylic acid, 2-[hydroxyamino)carbonyl]-1-[4-[2-methylquinolin-4-y)methoxy]phenyl]methyl], methyl ester, (1R, 2S)
02

Targets

ADAM17 (A disintegrin and metalloprotease 17)

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