N-DEVD-N′-morpholinecarbonyl-rhodamine 110: novel caspase-3 fluorogenic substrates for cell-based apoptosis assay

• Published in: Bioorganic & medicinal chemistry letters 2005-05, Vol.15 (9), p.2335-2338
• Main Authors: Wang, Zhi-Qiang, Liao, Jinfang, Diwu, Zhenjun
• Format: Article
• Language: English
• Subjects: Ageing, cell death; Analytical, structural and metabolic biochemistry; Apoptosis; Biological and medical sciences; Caspase; Caspase 3; Caspases - metabolism; Cell physiology; Enzymes and enzyme inhibitors; Fluorescent; Fluorogenic substrates; Fundamental and applied biological sciences. Psychology; HTS; Humans; Hydrolases; Indicators and Reagents; Kinetics; Models, Molecular; Molecular and cellular biology; Molecular Structure; Morpholines - chemical synthesis; Morpholines - chemistry; Morpholines - pharmacology; Oligopeptides - chemical synthesis; Oligopeptides - chemistry; Oligopeptides - pharmacology; Recombinant Proteins - metabolism; Rhodamines - chemical synthesis; Rhodamines - chemistry; Rhodamines - pharmacology; Substrate Specificity; Synthesis
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2005.02.081

The title compound is a single step cleavage fluorogenic substrate and has significantly higher enzyme turnover rate and sensitivity than existing fluorogenic substrates for detecting caspase-3 activity both in solution and living cells. A novel caspase-3 substrate N-Ac-DEVD-N′-MC-R110, which is a fluorogenic substrate cleavable in a single step, has been prepared. It has a significantly higher enzyme turnover rate and sensitivity for detecting caspase-3 activity both in solution and living cells than existing fluorogenic substrates.