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 99.94%
    Sitagliptin (MK-0431) is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin 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 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 shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin can be used for the study of 1-type and 2-type diabetes.
    Sitagliptin
  • HY-13233A
    Talabostat mesylate
    		Inhibitor 98.35%
    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-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-10284
    Linagliptin
    		Inhibitor 99.74%
    Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM.
    Linagliptin
  • HY-15695
    Puromycin aminonucleoside
    		Inhibitor 99.86%
    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-W198345
    Val-Pyrrolidide hydrochloride
    		Inhibitor 99.52%
    Val-Pyrrolidide hydrochloride (compound 9) is a DPIV inhibitor. Val-Pyrrolidide hydrochloride can prevent N-terminal truncation of the peptide Gln3-Aβ(1–11)[1].
    Val-Pyrrolidide hydrochloride
  • HY-P60234A
    AGFAGDDAPR
    		Inhibitor
    AGFAGDDAPR is a bioactive peptide that is a competitive and orally effective inhibitor of dipeptidyl peptidase-IV (DPP-IV). AGFAGDDAPR can enhance the level of GLP-1 in the body by inhibiting DPP-IV, thereby stimulating insulin secretion, improving β-cell function, and inhibiting abnormal proliferation of α-cells, exerting anti-diabetic effects. AGFAGDDAPR can be used for research on type 2 diabetes.
    AGFAGDDAPR
  • HY-P4633A
    D-γ-Glu-Tyr
    		Inhibitor 99.70%
    D-γ-Glu-Tyr is a D-isomer of γ-Glu-Tyr (HY-P4633), the difference being the γ-Glu content.γ-Glu-Tyr, a competitive inhibitor of dipeptidyl peptidase-IV (DPP-IV) (IC50=6.77 mM), is a potentially functional component of the type 2 diabetes diet.
    D-γ-Glu-Tyr
  • HY-111174
    Diprotin A
    		Inhibitor 99.90%
    Diprotin A (Ile-Pro-Ile) is an inhibitor of dipeptidyl peptidase IV (DPP-IV).
    Diprotin A
  • HY-13749A
    Sitagliptin phosphate
    		Inhibitor 99.88%
    Sitagliptin (MK-0431) phosphate is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin phosphate 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 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 shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin phosphate can be used for the study of 1-type and 2-type diabetes.
    Sitagliptin phosphate
  • HY-14291
    Vildagliptin
    		Inhibitor 99.93%
    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 98.50%
    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-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-A0023A
    Alogliptin
    		Inhibitor 99.93%
    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-119244
    Gly-Pro-pNA hydrochloride
    		99.92%
    Gly-Pro-pNA hydrochloride is a chromogenic peptide substrate that can be cleaved by the circulating enzyme dipeptidyl peptidase IV (DPP IV). Gly-Pro-pNA hydrochloride is mainly used to detect the activity of aminopeptidases such as DPP IV. Gly-Pro-pNA hydrochloride can be investigated as an experimental antidiabetic agent.
    Gly-Pro-pNA hydrochloride
  • HY-14806A
    Teneligliptin hydrobromide
    		Inhibitor 99.99%
    Teneligliptin (MP-513) hydrobromide is an orally active and selective dipeptidyl peptidase 4 (DPP-4) inhibitor (IC50s: 0.37 and 0.29 nM for the human and rat DPP-4, respectively). Teneligliptin hydrobromide improves blood glucose levels and can be used in researches related to type 2 diabetes mellitus.
    Teneligliptin hydrobromide
  • HY-14806
    Teneligliptin
    		Inhibitor 99.79%
    Teneligliptin (MP-513) hydrobromide hydrate is an orally active and selective dipeptidyl peptidase 4 (DPP-4) inhibitor (IC50s: 0.37 and 0.29 nM for the human and rat DPP-4, respectively). Teneligliptin hydrobromide hydrate improves blood glucose levels and can be used in researches related to type 2 diabetes mellitus.
    Teneligliptin
  • HY-15981
    Omarigliptin
    		Inhibitor 99.96%
    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-15408
    Trelagliptin
    		Inhibitor 99.81%
    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
  • HY-P4342
    Gly-Arg-AMC
    		Substrate 99.37%
    Gly-Arg-AMC is a peptide substrate of DPAP1.
    Gly-Arg-AMC
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Dipeptidyl Peptidase Isoform Comparison

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