The DPPIV Drug Discovery Kit is a complete assay system designed to screen DPPIV inhibitors, 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. The kit is useful to screen inhibitors of DPPIV, a potential therapeutic target. A DPPIV inhibitor, P32/98 (KI=130 nM12), is included for use as a control. Other DPP enzymes are available for specificity profiling.
Colorimetric detection, Fluorescence microscopy, HTS
DPPIV enzyme (human, recombinant), pNA substrate, Calibration standard (p-nitroaniline), AMC substrate, Calibration standard (7-Amino-4-methylcoumarin), Inhibitor, Assay Buffer, ½-volume clear microplate