KLK2 Fluorogenic Assay Kit

The KLK2 Fluorogenic Assay Kit is designed to measure KLK2 (Kallikrein-2) protease activity for screening and profiling applications. The assay kit comes in a convenient 96-well format, with enough recombinant KLK2 (amino acids 25-261), fluorogenic AMC-based peptide substrate, and assay buffer for 100 enzyme reactions. Figure 1: Illustration of the assay principle. A peptide substrate conjugated to AMC is incubated with KLK2. The conjugated AMC displays only weak fluorescence. Upon proteolysis, AMC is no longer quenched and exhibits strong blue fluorescence. The increase in fluorescence is proportional to the KLK2 activity. Need us to run inhibitor screens or profile your compounds against KLK2? Check out our Protease Screening Services. Kallikrein-2 (KLK2) is a trypsin-like serine protease. This protein is a member of the glandular kallikrein family and is critical in the enzymatic process as it selectively cleaves the Met-Lys and Arg-Ser bonds in kininogen, thereby releasing Lys-bradykinin. This proteolytic activity contributes to the production of bradykinin, a bioactive peptide with multiple roles in regulating blood pressure, inflammation, and vascular permeability. It is expressed by prostate epithelial cells and is regulated by the androgen receptor (AR). Its expression in prostate adenocarcinoma is nearly ubiquitous, and high expression levels are maintained in metastatic castration-resistant PC (mCRPC). While traditionally seen as secreted only, it is also present on the cancer cell surface. Its pattern of expression makes it an ideal target in the treatment of mCRPC using novel therapies, such as radioligands and immune-based therapies (like bispecific T cell engagers). Pasritamig is a clinical-stage human bispecific antibody that simultaneously binds to CD3 on T cells and cell surface KLK2 on tumor cells, enhancing the cytotoxicity towards KLK2-expressing tumor cells and it is currently under clinical trial. A deeper understanding of the role of membrane-bound or intracellular KLK2 and investigation into therapies will bring benefit to prostate cancer patients.