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

Dipeptidyl Peptidase

DPP

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-13749
    Sitagliptin
    Inhibitor 99.76%
    Sitagliptin (MK-0431) is a potent and orally active inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts.
    Sitagliptin
  • HY-15695
    Puromycin aminonucleoside
    Inhibitor 99.90%
    Puromycin aminonucleoside (NSC 3056) is the aminonucleoside portion of the antibiotic puromycin, and used in nephrosis animal models. Puromycin aminonucleoside induces apoptosis. Puromycin aminonucleoside is a reversible inhibitor of dipeptidyl peptidase II and cytosol alanyl aminopeptidase. Puromycin aminonucleoside induces secretion of cell migrasome.
    Puromycin aminonucleoside
  • HY-13233A
    Talabostat mesylate
    Inhibitor 98.16%
    Talabostat mesylate (Val-boroPro mesylate; PT100 mesylate) is an orally active and nonselective dipeptidyl peptidase IV (DPP-IV) inhibitor (IC50 < 4 nM; Ki = 0.18 nM) and the first clinical inhibitor of fibroblast activation protein (FAP) (IC50 = 560 nM), inhibits DPP8/9 (IC50 = 4/11 nM; Ki = 1.5/0.76 nM), quiescent cell proline dipeptidase (QPP) (IC50 = 310 nM), DPP2, and some other DASH family enzymes. Antineoplastic and hematopoiesis- stimulating activities.
    Talabostat mesylate
  • HY-10284
    Linagliptin
    Inhibitor 99.91%
    Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM.
    Linagliptin
  • HY-101056
    Brensocatib
    Inhibitor 98.47%
    Brensocatib (AZD7986) is an oral dipeptidyl peptidase 1 (DPP1) inhibitor with pIC50s of 6.85, 7.6, 7.7, 7.8, and 7.8 in human, mouse, rat, dog and rabbit, respectively.
    Brensocatib
  • HY-163332
    MPO-IN-6
    Inhibitor
    MPO-IN-6 (compound ADC) is an electrophile with good antioxidant and anti-inflammatory properties. MPO-IN-6 is a myeloperoxidase (MPO), dipeptidyl peptidase-4 (DPP-4), and α-glucosidase (α-GD) inhibitor with IC50s of 10 μM, 31.02 μM, and 46.05 μM, respectively. MPO-IN-6 is a potential cardiovascular preventive agent.
    MPO-IN-6
  • HY-156846
    O-Benzoylhydroxylamine
    Inhibitor
    O-Benzoyl hydroxylamine is a DPP-IV inhibitor with anti-diabetic effects (WO2006034435A2).
    O-Benzoylhydroxylamine
  • HY-N2612
    O-Methyldauricine
    Inhibitor
    O-Methyldauricine is a selective microbial DPP4 inhibitor that can improve glucose tolerance in diabetic mice.
    O-Methyldauricine
  • HY-10285
    Saxagliptin
    Inhibitor 99.96%
    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
  • HY-14291
    Vildagliptin
    Inhibitor 99.61%
    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
  • HY-116304
    1G244
    Inhibitor 98.66%
    1G244 is a potent DPP8/9 inhibitor with IC50s of 12 nM and 84 nM, respectively. 1G244 does not inhibit DPPIV and DPPII. 1G244 induces apoptosis in multiple myeloma cells and has anti-myeloma effects.
    1G244
  • HY-13749A
    Sitagliptin phosphate
    Inhibitor 99.85%
    Sitagliptin phosphate (MK-0431 phosphate) is a potent inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts.
    Sitagliptin phosphate
  • HY-15981
    Omarigliptin
    Inhibitor
    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
  • HY-13749B
    Sitagliptin phosphate monohydrate
    Inhibitor 99.49%
    Sitagliptin phosphate monohydrate (MK-0431 phosphate monohydrate) is a potent inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts.
    Sitagliptin phosphate monohydrate
  • HY-14806
    Teneligliptin
    Inhibitor 99.85%
    Teneligliptin (MP-513) is a potent, orally available, competitive, and long-lasting DPP-4 inhibitor. Teneligliptin competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM.
    Teneligliptin
  • HY-111174
    Diprotin A
    Inhibitor 99.58%
    Diprotin A (Ile-Pro-Ile) is an inhibitor of dipeptidyl peptidase IV (DPP-IV).
    Diprotin A
  • HY-A0023
    Alogliptin Benzoate
    Inhibitor 99.99%
    Alogliptin Benzoate (SYR-322) is a potent, selective and orally active inhibitor of DPP-4 with an IC50 of <10 nM, and exhibits greater than 10,000-fold selectivity over DPP-8 and DPP-9. Alogliptin Benzoate can be used for the research of type 2 diabetes.
    Alogliptin Benzoate
  • HY-A0023A
    Alogliptin
    Inhibitor 99.92%
    Alogliptin (SYR-322 free base) is a potent, selective and orally active inhibitor of DPP-4 with an IC50 of <10 nM, and exhibits greater than 10,000-fold selectivity over DPP-8 and DPP-9. Alogliptin can be used for the research of type 2 diabetes.
    Alogliptin
  • HY-B0422
    Nateglinide
    Inhibitor 99.51%
    Nateglinide, a D-phenylalanine derivative, is an orally active and short-acting insulinotropic agent and a DPP IV inhibitor. Nateglinide inhibits ATP-sensitive K+ channels in pancreatic β-cells. Nateglinide is used for the treatment of type 2 (non-insulin-dependent) diabetes mellitus.
    Nateglinide
  • HY-15408
    Trelagliptin
    Inhibitor 99.54%
    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
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