ADAM17 fluorometric drug discovery kit

The ADAM17 Fluorometric (also known as fluorimetric) Drug Discovery Kit is a complete assay system designed to screen ADAM17 (TACE) inhibitors using a quenched fluorogenic peptide: Mca-PLAQAV-Dpa-RSSSR-NH₂. Mca fluorescence is quenched by the Dpa group until cleavage by proteases separates the two moieties. The assays are performed in a convenient 96-well microplate format.  The kit is useful to screen inhibitors of ADAM17, a potential therapeutic target. The compound GM6001 is also included as a prototypic control inhibitor.

TACE/ADAM17 (Tumor necrosis factor-α-converting enzyme; A Disintegrin And Metalloproteinase 17) is a soluble or membrane-bound metalloproteinase primarily responsible for activation of proTNF-α, while also targeting proteins such as fractalkine, amyloid precursor proteins, and CD40. ADAM17/TACE is involved in cancer, vascular disorders, and inflammatory diseases such as rheumatoid arthritis and focal ischemic injury. The catalytic domain of ADAM17/TACE is able to cleave proTNF-α and is used in inhibitor screening.