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-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-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 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-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-10284
    Linagliptin
    		Inhibitor 99.91%
    Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM.
    Linagliptin
  • HY-101056
    Brensocatib
    		Inhibitor 99.88%
    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-117985A
    Evogliptin hydrochloride
    		Inhibitor
    Evogliptin hydrochloride (DA-1229 hydrochloride) is an orally available DPP4 inhibitor with significant and durable hypoglycemic effects in mouse models. Evogliptin hydrochloride also inhibits the generation of inflammatory and fibrotic signals in hepatocytes by inducing autophagy. Evogliptin hydrochloride can be used in the research of type 2 diabetes, osteoporosis, renal impairment and chronic liver inflammation.
    Evogliptin hydrochloride
  • HY-161428
    ZINC000003015356
    		Inhibitor
    ZINC000003015356 is a DPP4 inhibitor.
    ZINC000003015356
  • HY-158315
    NZ-97
    		Inhibitor
    NZ-97 is an inhibitor for dipeptidyl peptidase 4 (DPP4) with an IC50 of 18 nM. NZ-97 exhibits a low initial plasma exposure with Cmax of 0.13 µM, which is eliminated in 8 h. NZ-97 ameliorates damage in the Lipopolysaccharides (HY-D1056)-induced lung injury and Bleomycin (HY-108345)-induced lung fibrosis in mice model.
    NZ-97
  • 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-111174
    Diprotin A
    		Inhibitor 99.58%
    Diprotin A (Ile-Pro-Ile) is an inhibitor of dipeptidyl peptidase IV (DPP-IV).
    Diprotin A
  • 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-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-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-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-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-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-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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Dipeptidyl Peptidase Isoform Comparison

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