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.

Dipeptidyl Peptidase Related Products (47):

Cat. No. Product Name Effect Purity
  • HY-13233A
    Talabostat mesylate Inhibitor ≥98.0%
    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-15695
    Puromycin aminonucleoside Inhibitor ≥98.0%
    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.
  • HY-13749
    Sitagliptin 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
    Linagliptin Inhibitor 99.97%
    Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM.
  • HY-14291
    Vildagliptin 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-14892
    Gemigliptin Inhibitor
    Gemigliptin (LC15-0444 ) is a highly selective, reversible and competitive dipeptidyl peptidase-4 (DPP-4) inhibitor, with an IC50 of 10.3 nM for human recombinant DPP-4. Gemigliptin exhibits potent anti-glycation properties. Gemigliptin can be used for the research of advanced glycation end products (AGE)-related diabetic complications.
  • HY-16448
    Saxagliptin hydrochloride Inhibitor
    Saxagliptin hydrochloride (BMS-477118 hydrochloride) is a potent, selective, reversible, competitive and orally active dipeptidyl peptidase-4 (DPP-4) (Ki = 0.6-1.3 nM) inhibitor. Saxagliptin hydrochloride has the peotential for type 2 diabetes mellitus research.
  • HY-112668A
    Retagliptin Inhibitor
    Retagliptin (SP2086) is a selective, competitive and orally active dipeptidyl peptidase-4 (DPP-4) inhibitor. Retagliptin can be used for type 2 diabetes mellitus (T2DM) 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-101056
    Brensocatib 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-10285
    Saxagliptin Inhibitor
    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-14806
    Teneligliptin Inhibitor 99.57%
    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-14877
    Anagliptin Inhibitor
    Anagliptin is a highly selective, potent inhibitor of dipeptidyl peptidase 4 (DPP-4), with an IC50 of 3.8 nM, and less selective at DPP-8/9 (IC50, 68, 60 nM, respectively).
  • HY-116304
    1G244 Inhibitor ≥98.0%
    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-111174A
    Diprotin A TFA Inhibitor 98.80%
    Diprotin A TFA (Ile-Pro-Ile TFA) is an inhibitor of dipeptidyl peptidase IV (DPP-IV).
  • 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-15981
    Omarigliptin Inhibitor
    Omarigliptin(MK-3102) is a potent, selective and long-acting DPP-4 inhibitor with IC50 of 1.6 nM; highly selective over all proteases tested (IC50 > 67 μM).
  • HY-15408
    Trelagliptin 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).
  • HY-15408A
    Trelagliptin succinate Inhibitor 99.96%
    Trelagliptin (SYR-472) succinate 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).
  • HY-14806A
    Teneligliptin hydrobromide Inhibitor ≥99.0%
    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.
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