General description

Cathepsin K (CTSK; EC 3.4.22.38) is a lysosomal cysteine proteinase expressed predominantly in the osteoclasts. It exhibits potent collagenase activity and is involved in bone remodeling and resorption. Mutations in CTSK gene result in pycnodysostosis characterized by osteosclerosis and short stature.

Principle

The Cathepsin K Inhibitor Screening Kit is a simple assay for screening potential inhibitors of CTSK. CTSK activity is measured by cleaving a synthetic 7-amino-4-trifluoromethylcoumarin (AFC)-based substrate to yield AFC, a fluorescent product (λ_ex = 400/ λ_em = 505 nm), proportional to the enzymatic activity present.

Suitability

Suitable for the screening of inhibitors of Cathepsin K.