||Dipeptidyl peptidase-4 (DPP4) inhibitors have emerged as a new class of oral antidiabetic agents. These inhibitors promote glucose homeostasis by inhibiting degradation of glucosedependent insulinotropic polypeptide and glucagon-like peptide-1 by DPP4. Glucagon-like peptide-1 extends the action of insulin while suppressing the release of glucagon. In DPP4 Inhibitor Screening Kit, DPP4 cleaves a substrate to release a quenched fluorescent group (Em/Ex = 360/460 nm). In presence of a DPP4 inhibitor, the cleavage will be inhibited. The kit provides a rapid, simple, sensitive, and reliable test, as well as, suitable for high throughput screening of DPP4 inhibitors. Sitagliptin is included as a control inhibitor to compare the efficacy of the test inhibitors.