DPPIV Drug Discovery Kit is designed to screen DPPIV inhibitors. Research Use Only. Not for Use in Diagnostic Procedures.
Regulatory Status
Research Use Only. Not for Use in Diagnostic Procedures.
Product Distribution
Available Worldwide
Sizes
96 Tests
Sample Types
See Package Insert
Inc Time Overnight
No
Inc Time See Protocol
No
Additional Information
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.