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N-Ac-DEVD-N'-(Polyfluorobenzoyl)-R110: Novel Cell-Permeable Fluorogenic Caspase Substrates for the Detection of Caspase Activity and Apoptosis

N-Ac-DEVD-N'-(Polyfluorobenzoyl)-R110: Novel Cell-Permeable Fluorogenic Caspase Substrates for the Detection of Caspase Activity and Apoptosis

Han-Zhong Zhang, Shailaja Kasibhatla, John Guastella, Ben Tseng, John Drewe, Sui Xiong Cai

Bioconjug Chem. Mar-Apr 2003;14(2):458-63.

PMID: 12643757

Abstract:

N-Pentafluorobenzoyl-R110 (1a) and N-(2,3,4,5-tetrafluorobenzoyl)-R110 (1b) with enhanced cell retention properties, were prepared from rhodamine 110 (R-110) and the corresponding polyfluorobenzoyl chloride. N-Ac-DEVD-N'-pentafluorobenzoyl-R110 (3a) and N-Ac-DEVD-N'-(2,3,4,5-tetrafluorobenzoyl)-R110 (3b) were prepared as tetrapeptide substrates for caspases. Substrate 3b was efficiently cleaved by human recombinant caspase-3 in an enzyme assay. Substrate 3b also was efficiently cleaved in cell-based apoptosis assays. After cleavage in apoptotic cells by activated caspases, the substrate becomes fluorescent as measured by flow cytometry. These substrates should prove useful in cell-based assays for studying apoptosis inducers and inhibitors.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP13558311	Rhodamine 110 chloride		13558-31-1	Price

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