The DPPIV Drug Discovery Kit is a complete assay system designed to screen DPPIV inhibitors, a potential therapeutic target, providing enough material to perform at least 96 assays.

DPPIV (DPP4, CD26) is a member of the class of proteases known as prolyl peptidases, which cleave proteins after proline residues and is thought to play roles in diabetes, cancer, and autoimmune diseases, making it a target for drug discovery.

The kit contains both a chromogenic substrate (H-Gly-Pro-pNA; Km=114 µm) and a fluorogenic substrate (H-Gly-Pro-AMC; Km=50 µm).

Cleavage of the p-nitroaniline (pNA) from the colorimetric substrate increases absorbance at 405 nm. The fluorimetric assay is based on the cleavage of 7-amino-4-methylcoumarin (AMC) moiety from the C-terminus of the peptide substrate, which increases its fluorescence intensity at 460 nm.

A DPPIV inhibitor, P32/98 (KI=130 nm12), is included for use as a control. Other DPP enzymes are available for specificity profiling.