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

Dipeptidyl Peptidase


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
  • 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.
  • HY-13233A
    Talabostat mesylate
    Inhibitor 99.05%
    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.
  • HY-13749
    Inhibitor 99.72%
    Sitagliptin (MK-0431) is a potent inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts.
  • HY-10284
    Inhibitor 99.97%
    Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM.
  • HY-101056
    Inhibitor 99.66%
    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.
  • HY-117985
    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.
  • HY-148190
    Sheng Gelieting
    Sheng Gelieting (CGT-8012) is a dipeptidy peptidase-IV enzyme (DP-IV) inhibitor. Sheng Gelieting has great DP-IV inhibition activity with an IC50 value of 87 nM. Sheng Gelieting can be used for curing or preventing diseases relevant to the dipeptidy peptidase-IV enzyme, such as the diabetes, particularly the II-type diabete.
  • HY-147401
    Sitagliptin fenilalanil
    Sitagliptin fenilalanil is a dipeptidyl aminopeptidase 4 (DPP-4) inhibitor.
  • HY-116304
    Inhibitor 98.55%
    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.
  • HY-14291
    Inhibitor 98.18%
    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.
  • HY-10285
    Inhibitor 99.39%
    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.
  • HY-13749B
    Sitagliptin phosphate monohydrate
    Inhibitor 99.62%
    Sitagliptin phosphate monohydrate (MK-0431 phosphate monohydrate) is a potent inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts.
  • HY-111174A
    Diprotin A TFA
    Inhibitor 99.14%
    Diprotin A TFA (Ile-Pro-Ile TFA) is an inhibitor of dipeptidyl peptidase IV (DPP-IV).
  • HY-14877
    Anagliptin (SK-0403) is a highly selective, potent, orally active inhibitor of dipeptidyl peptidase 4 (DPP-4), with an IC50 of 3.8 nM, and less selective at DPP-8 and DDP-9 with IC50s of 68 nM and 60 nM, respectively.
  • HY-15981
    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.
  • HY-14806
    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.
  • HY-14806A
    Teneligliptin hydrobromide
    Inhibitor 99.95%
    Teneligliptin (MP-513) hydrobromide is a potent chemotype prolylthiazolidine-based DPP-4 inhibitor, which competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM.
  • HY-112668
    Retagliptin phosphate
    Inhibitor 99.89%
    Retagliptin phosphate (SP2086 phosphate) is a selective, competitive and orally active dipeptidyl peptidase-4 (DPP-4) inhibitor. Retagliptin phosphate can be used for type 2 diabetes mellitus (T2DM) research.
  • HY-A0023
    Alogliptin Benzoate
    Inhibitor 99.96%
    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.
  • HY-15408
    Inhibitor 99.80%
    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).
Cat. No. Product Name / Synonyms Species Source