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-175590
    DPP-4-IN-17
    		Inhibitor
    DPP-4-IN-17 is an orally active and selective dipeptidyl peptidase-4 (DPP-4) inhibitor with an IC50 value of 0.12 nM. DPP-4-IN-17 increases the enzyme's Km value (75.73 μM vs. 27.18 μM of substrate alone) and reduces catalytic efficiency. DPP-4-IN-17 reduces blood glucose levels and reverses weight loss in Streptozotocin (STZ) (HY-13753)/Nicotinamide (NA) (HY-B0150)-induced diabetic rats. DPP-4-IN-17 can be used for the study of type 2 diabetes mellitus (T2DM).
    DPP-4-IN-17
  • HY-14291R
    Vildagliptin (Standard)
    		Inhibitor
    Vildagliptin (Standard) is the analytical standard of Vildagliptin. This product is intended for research and analytical applications. 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 (Standard)
  • HY-13749S3
    Sitagliptin-d6
    		Inhibitor
    Sitagliptin-d6 (MK-0431-d6) is deuterium labeled Sitagliptin (HY-13749). Sitagliptin 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-d<sub>6</sub>
  • HY-10285S1
    (rel)-Saxagliptin-13C,d2 TFA
    		Inhibitor
    (rel)-Saxagliptin-13C,d2 ((rel)-BMS-477118-13C,d2) TFA is 13C-labeled Saxagliptin (HY-10285).
    (rel)-Saxagliptin-<sup>13</sup>C,d<sub>2</sub> TFA
  • HY-N14989A
    Fluostatin A sodium
    		Inhibitor
    Fluostatin A sodium is a dipeptidyl peptidaseIII inhibitor with an IC50 of 0.44 μg/mL. Fluostatin A can be extracted from Streptomyces sp. TA-3391.
    Fluostatin A sodium
  • HY-N14989
    Fluostatin A
    		Inhibitor
    Fluostatin A inhibits the ability of DPP-III, and with arginyl-arginine-2-naphthalene formamide as the substrate, the IC50 is 0.44 μg/mL.
    Fluostatin A
  • HY-14806S2
    Teneligliptin-d5
    		Inhibitor
    Teneligliptin-d5 (MP-513-d5) is deuterium labeled Teneligliptin. 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-d<sub>5</sub>
  • HY-12733
    AZD5248
    		Inhibitor
    AZD5248 is a dipeptidyl peptidase 1 (DPP1) inhibitor that can be used for the research of chronic obstructive lung disease.
    AZD5248
  • HY-19859
    AMG-222 tosylate
    AMG-222 (tosylate) is a DPP-IV inhibitor that can be used in the research of type II diabete.
    AMG-222 tosylate
  • HY-N15181
    Fluostatin B
    		Inhibitor
    Fluostatin B is a dipeptidyl peptidase 3 (DPP-3) inhibitor with an IC50 value of 24 µg/mL. Fluostatin B is a fluorenone, which is found in Streptomyces.
    Fluostatin B
  • HY-16656
    BMS-767778
    		Inhibitor
    BMS-767778 is a selective DPP4 inhibitor, with a Ki of 0.9 nM.
    BMS-767778
  • HY-N15105
    Acetyl-L-Ieucyl-L-argininal
    Acetyl-L-Ieucyl-L-argininal shows inhibition of peptidyl amin-peptidase III activity.
    Acetyl-L-Ieucyl-L-argininal
  • HY-134666A
    Dioctatin A hydrochloride
    		Inhibitor
    Dioctatin A hydrochloride is a metabolite of Streptomyces and an inhibitor of human dipeptidyl aminopeptidase II. Dioctatin A hydrochloride can inhibit aflatoxin production by Aspergillus parasiticus with an IC50 of 4.0 μM. Dioctatin A hydrochloride can reduce the mRNA levels of aflatoxin biosynthetic genes and the regulatory gene aflR, inhibit conidiation and decrease the mRNA level of the brlA gene, and also promote kojic acid production. In addition, Dioctatin A hydrochloride can inhibit sterigmatocystin production. Dioctatin A hydrochloride has pleiotropic regulatory effects on the production and differentiation of fungal secondary metabolites.
    Dioctatin A hydrochloride
  • HY-14877S1
    Anagliptin-d7
    		Inhibitor
    Anagliptin-d7 (SK-0403-d7) is deuterium labeled Anagliptin. 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.
    Anagliptin-d<sub>7</sub>
  • HY-A0299A
    H-Gly-Pro-Hyp-OH acetate
    		Inhibitor
    H-Gly-Pro-Hyp-OH acetate is a dipeptidyl peptidase 4 (DPP-4) inhibitor with an IC50 value of 2.51 mM. H-Gly-Pro-Hyp-OH acetate is promising for research of diabetes.
    H-Gly-Pro-Hyp-OH acetate
  • HY-10284R
    Linagliptin (Standard)
    		Inhibitor
    Linagliptin (Standard) is the analytical standard of Linagliptin. This product is intended for research and analytical applications. Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM.
    Linagliptin (Standard)
  • HY-10285S2
    Saxagliptin-13C2
    		Inhibitor
    Saxagliptin-13C2 (BMS-477118-13C2) is 13C labeled Saxagliptin. 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-<sup>13</sup>C<sub>2</sub>
  • HY-Z3637
    (–)-Sitagliptin carbamoyl glucuronide
    		Control
    (–)-Sitagliptin carbamoyl glucuronide is a minor metabolite of the dipeptidyl peptidase 4 (DPP-4) inhibitor Sitagliptin (HY-13749).
    (–)-Sitagliptin carbamoyl glucuronide
  • HY-A0023AR
    Alogliptin (Standard)
    		Inhibitor
    Alogliptin (Standard) is the analytical standard of Alogliptin. This product is intended for research and analytical applications. 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 (Standard)
  • HY-14877R
    Anagliptin (Standard)
    		Inhibitor
    Anagliptin (Standard) is the analytical standard of Anagliptin. This product is intended for research and analytical applications. 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.
    Anagliptin (Standard)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Dipeptidyl Peptidase Isoform Comparison

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