2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. Dipeptidyl Peptidase

Dipeptidyl Peptidase

DPP

Dipeptidyl Peptidase

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Dipeptidyl Peptidases are widely distributed exopeptidases that possess central role in proteolysis. The dipeptidyl peptidase family, including DPP-IV DPP7, DPP8, DPP9, fibroblast activation protein and others, cleave the peptide bond after the penultimate proline residue and are drug target rich.

DPP-IV (DPP4 or CD26) is a serine protease detected on several immune cells and on epithelial cells of various organs. Besides the membrane-bound enzyme, a catalytically active soluble form is detected in several body fluids. Both variants cleave off dipeptides from the N-termini of various chemokines, neuropeptides, and hormones. DPP IV plays a key role in immune-regulation, inflammation, oxidative stress, cell adhesion, and apoptosis by targeting different substrates. DPP IV inhibitors are commonly used as hypoglycemic agents.

DPP8 and DPP9 show DPPIV-like activity and share a very high-sequence similarity to each other. DPP8 and DPP9 are intracellular N-terminal dipeptidyl peptidases (preferentially postproline) associated with pathophysiological roles in immune response and cancer biology.

Dipeptidyl Peptidase Isoform Specific Products:

Dipeptidyl Peptidase Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-P991050
    Procizumab
    		Inhibitor
    Procizumab (AK-1967) is a humanized IgG1 antibody that targets dipeptidyl peptidase 3 (DPP3). Procizumab has the potential for the study of sepsis. The isotype control for Procizumab can refer to Human IgG1 kappa, Isotype Control (HY-P99001).
    Procizumab
  • HY-15408R
    Trelagliptin (Standard)
    		Inhibitor
    Trelagliptin (Standard) is the analytical standard of Trelagliptin. This product is intended for research and analytical applications. Trelagliptin (SYR-472) is a potent, orally active and highly selective DPP-4 inhibitor with an IC50 of 4 nM. Trelagliptin succinate improves glycemic control in vivo and can be used for the study of type 2 diabetes mellitus (T2DM).
    Trelagliptin (Standard)
  • HY-N4069
    Lupinalbin A
    		Inhibitor
    Lupinalbin A (Boeravinone L) is a dipeptidyl peptidase 4 (DPP4) and α-glucosidase inhibitor with IC50 values ​​of 45.2 and 53.4 µM, respectively. Lupinalbin A exhibits antidiabetic activity.
    Lupinalbin A
  • HY-14291S
    Vildagliptin-d3
    		Inhibitor
    Vildagliptin-d3 is the deuterium labeled Vildagliptin. Vildagliptin (LAF237) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin possesses excellent oral bioavailability and potent antihyperglycemic activity.
    Vildagliptin-d<sub>3</sub>
  • HY-135534
    Lysine 4-nitroanilide
    Lysine 4-nitroanilide is an amino acid derivative of 4-nitroanilide (component C1 substrate) used in enzymology research and as a substrate for arylamidase/DPP-3 activity assays.
    Lysine 4-nitroanilide
  • HY-15981R
    Omarigliptin (Standard)
    		Inhibitor
    Omarigliptin (Standard) is the analytical standard of Omarigliptin. This product is intended for research and analytical applications. Omarigliptin (MK-3102) is a potent, selective, orally active and cross the blood-brain barrier dipeptidyl peptidase 4 (DPP-4) inhibitor. Omarigliptin shows anti-parkinsonian activity. Omarigliptin has the neuroprotective effect to improve diabetes-associated cognitive dysfunction.
    Omarigliptin (Standard)
  • HY-119266
    HTS13517
    		Inhibitor
    HTS13517 is a DPP4 inhibitor, with an IC50 of 10.73 μM.
    HTS13517
  • HY-13749BR
    Sitagliptin phosphate monohydrate (Standard)
    		Inhibitor
    Sitagliptin (MK-0431) phosphate monohydrate (Standard) is the analytical standard of Sitagliptin phosphate monohydrate (HY-13749B). This product is intended for research and analytical applications. Sitagliptin phosphate monohydrate is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin phosphate monohydrate blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin phosphate monohydrate can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin phosphate monohydrate shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin phosphate monohydrate can be used for the study of 1-type and 2-type diabetes.
    Sitagliptin phosphate monohydrate (Standard)
  • HY-10285R
    Saxagliptin (Standard)
    		Inhibitor
    Saxagliptin (Standard) is the analytical standard of Saxagliptin. This product is intended for research and analytical applications. Saxagliptin (BMS-477118) is a potent, selective, reversible, competitive and orally active dipeptidyl peptidase-4 (DPP-4) (Ki = 0.6-1.3 nM) inhibitor. Saxagliptin has the peotential for type 2 diabetes mellitus research.
    Saxagliptin (Standard)
  • HY-109060
    Garvagliptin
    		Inhibitor
    Garvagliptin (ZYDPLA1) is an orally active, competitive and long acting DPP4 Inhibitor, with an IC50 of 2.99 nM against human recombinant DPP IV. Garvagliptin (ZYDPLA1) exhibits antihyperglycemic effect.
    Garvagliptin
  • HY-174832
    DPP-4-IN-16
    		Inhibitor
    DPP-4-IN-16 (Compound 92) is a potent dipeptidyl peptidase-4 (DPP-4) inhibitor (IC50=0.8 nM). DPP-4-IN-16 inhibits DPP-4-mediated degradation of incretins (e.g., GLP-1 and GIP) to promote insulin secretion and reduce blood glucose. DPP-4-IN-16 is promising for research of type 2 diabetes.
    DPP-4-IN-16
  • HY-10284S4
    Linagliptin-d5
    		Inhibitor
    Linagliptin-d5 (BI 1356-d5) is deuterium labeled Linagliptin. Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM.
    Linagliptin-d<sub>5</sub>
  • HY-U00346A
    TS-021
    		Inhibitor
    TS-021 is a selective，orally active，reversible and long-acting DPP-IV inhibitor，and exhibits significant inhibition selectivity against DPP-8 (> 600 fold)，DPP-9 (> 1200 fold) and other peptidases (> 15,000 fold). TS-021 inhibits DPP-IV activity in human plasma with an IC50 value of 5.34 nM. TS-021 has long-term persistent plasma drug concentration and potent antihyperglycemic activity，and increases in the active form of GLP-1.
    TS-021
  • HY-14291S5
    Vildagliptin-d6
    		Inhibitor
    Vildagliptin-d6 (LAF237-d6 ) is deuterium labeled Vildagliptin. Vildagliptin (LAF237) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin possesses excellent oral bioavailability and potent antihyperglycemic activity.
    Vildagliptin-d<sub>6</sub>
  • HY-13749D
    (Rac)-Sitagliptin
    		Inhibitor
    (Rac)-Sitagliptin is an isoform of Sitagliptin (HY-13749), which is a potent and orally active inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts.
    (Rac)-Sitagliptin
  • HY-117985S
    Evogliptin-d9
    		Inhibitor
    Evogliptin-d9 (DA-1229-d9) is deuterium labeled Evogliptin. Evogliptin (DA-1229) is an orally active DPP4 inhibitor with significant and sustained hypoglycaemic effects in mouse models. Evogliptin also inhibits the production of inflammatory and fibrotic signals in hepatocytes by inducing autophagy. Evogliptin can be used in studies of type 2 diabetes, osteoporosis, renal impairment and chronic liver inflammation.
    Evogliptin-d<sub>9</sub>
  • HY-175226
    DPP8/9-IN-2
    		Inhibitor
    DPP8/9-IN-2 (Compound 21) is a DPP8/9 inhibitor with IC50 values of 0.22 nM and 3 nM, respectively, and Ki values of 2.9 nM and 6 nM, respectively . DPP8/9-IN-2 has certain cardiotoxicity, with IC50 values of 0.7 μM, 29.0 μM and 27.7 μM for hERG potassium channel, Nav1.5 sodium channel and Cav1.2 calcium channel, respectively. DPP8/9-IN-2 can be used in the research of diseases such as tumors.
    DPP8/9-IN-2
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Dipeptidyl Peptidase Isoform Comparison

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