ADAM17 Fluorogenic Assay Kit

The ADAM17 Fluorescent Assay Kit is provided in a convenient 96-well format, with purified ADAM17, ADAM Fluorogenic Substrate, and ADAM assay buffer for 96 enzyme reactions. The key to the ADAM17 Fluorescent Assay Kit is the fluorogenic substrate. Using this kit, only one simple step on a microtiter plate is required for ADAM17 reactions. A sample containing ADAM17 is incubated in a reaction mixture with the fluorogenic substrate and fluorescence (λex=485±10 nm, λem=530±10 nm) is measured using a plate reader.

Study enzyme kinetics and screen small molecule inhibitors of ADAM17 for drug discovery and high throughput screening (HTS) applications.
ADAM17 (A disintegrin and a metalloprotease 17), also known as TACE (TNF-α converting enzyme), is one of the 22 members of the ADAM family of proteins found in humans and part of the zinc protease superfamily. It is involved in development, immunity, inflammation and tumorigenesis. ADAM17 is found in the brain, heart, kidney and skeletal muscle, amongst others. It has more than 80 substrates, ranging from EGFR (epidermal growth factor receptor) ligands, TNF-α (tumor necrosis factor alpha) to adhesion molecules and amyloid precursor protein, and it is thus involved in multiple pathways. Its activity is highly regulated, with low activity resulting in issues with regeneration due to low EFGR signaling, while increased activity can lead to tumor development. This protein is formed in the ER (endoplasmic reticulum) as a proform and matures in the Golgi apparatus where the prodomain is cleaved by pro-protein convertases. Patients with RA (rheumatoid arthritis) have elevated activity of ADAM17 in the synovial tissue. Because of the roles it plays, targeting this protein in diseased tissues without affecting the healthy tissues is a major concern. The development of therapies targeting this protein in specific tissues will no doubt result in advances in ADAM-17 related diseases.
Datasheet and Protocols may be found here.