Dipeptidyl Peptidase
DPP
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
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Dipeptidyl Peptidase Inhibitors
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Dipeptidyl Peptidase Antagonist
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Dipeptidyl Peptidase Activator
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Dipeptidyl Peptidase Controls
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Dipeptidyl Peptidase Substrates
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DPP IV/CD26 Proteins
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Dipeptidyl Peptidase Related Products (239)
Related Products (239)
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Recombinant Proteins (9)
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Antibodies (1)
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Dipeptidyl Peptidase Isoform Comparison
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Sitagliptin-d4 phosphate
0 ImagesSynonyms: MK-0431-d4 phosphateSitagliptin-d4 phosphate (MK-0431-d4) is the deuterium labeled Sitagliptin phosphate (HY-13749A). Sitagliptin 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.
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Saxagliptin hydrate
0 ImagesSynonyms: BMS-477118 hydrateSaxagliptin hydrate (BMS-477118 hydrate) is a potent, selective, reversible, competitive and orally active dipeptidyl peptidase-4 (DPP-4) (Ki = 0.6-1.3 nM) inhibitor. Saxagliptin hydrate has the peotential for type 2 diabetes mellitus research.
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Cichoriin
0 ImagesCichoriin is an orally active coumarin glycoside with broad biological activities. Cichoriin exhibits inhibitory activities against α-amylase, α-glucosidase, pancreatic lipase and DPP-IV, with IC50 values of 5.76, 2.94, 16.83 and 9.16 μg/mL, respectively. Cichoriin significantly improves metabolic dysfunction-associated steatohepatitis (MASH) in mice by activating the AMPK signaling pathway. Cichoriin upregulates PPAR-γ in adipose tissue and alleviates obesity and associated cardiorenal injury in rats. Cichoriin blocks monosodium urate crystal-induced activation of the NLRP3 inflammasome and cell pyroptosis by inhibiting P2Y14R (IC50 = 8.47 nM). In silico virtual screening reveals that Cichoriin has a strong binding affinity for SARS-CoV-2.
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Val-Pyrrolidide hydrochloride
0 ImagesVal-Pyrrolidide hydrochloride (compound 9) is a DPIV inhibitor. Val-Pyrrolidide hydrochloride can prevent N-terminal truncation of the peptide Gln3-Aβ(1–11)[1].
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Diprotin A TFA
0 ImagesSynonyms: Ile-Pro-Ile TFADiprotin A TFA (Ile-Pro-Ile TFA) is an inhibitor of dipeptidyl peptidase IV (DPP-IV).
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Diprotin B
0 ImagesDiprotin B is a dipeptidyl aminopeptidase IV (DPP IV) inhibitor. The apparent competitive inhibition of DPP-IV by the diprotins is a kinetic artifact, derived from the substrate-like nature of tripeptides containing a penultimate proline residue.
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Sitagliptin-d4 hydrochloride
0 ImagesCat. No.: HY-13749S1Purity: 99.22%Synonyms: MK-0431-d4 hydrochlorideSitagliptin-d4 hydrochloride is the deuterium labeled Sitagliptin hydrochloride (HY-13749E). Sitagliptin hydrochloride is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin hydrochloride 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 hydrochloride 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 hydrochloride shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin hydrochloride can be used for the study of 1-type and 2-type diabetes.
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Azaleatin
0 ImagesAzaleatin is an orally active inhibitor of hQC, NS2B-NS3 protease and E. coli β-glucuronidase, with IC50 values of 1.1 μM, 38.00 μg/mL and 0.57 μM, respectively. Azaleatin inhibits the activities of NF-κB, MyD88, JAK1, TLR4, STAT3, IL-1β, IL-6, COX-2, TNF-α and β-glucuronidase, blocks pro-inflammatory signaling pathways, reduces the levels of ROS, MDA and uric acid, elevates the levels of GPx, GSR, GST, SOD, CAT, HO-1 and GSH, scavenges free radicals and exerts reducing capacity. Azaleatin inhibits the expression of pro-apoptotic proteins Bax, Caspase-9 and Caspase-3, and upregulates the expression of anti-apoptotic protein Bcl-2. Azaleatin reduces the levels of cardiac injury markers, restores cardiac histological structure, inhibits Aβ aggregation, dengue protease activity, hepatic stellate cell proliferation and cancer cell growth, and also exhibits antibacterial activity. Azaleatin can be used in studies related to subchronic cardiotoxicity, Alzheimer's disease, dengue fever, hyperuricemia, liver fibrosis, gastric cancer and bacterial infections.
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NZ-97
0 ImagesCat. No.: HY-158315Purity: 99.43%NZ-97 is a locally deliverable, lung-retaining dipeptidyl peptidase 4 (DPP4) inhibitor with an IC50 of 18 nM. It exhibits selectivity for DPP8 and DPP9 (with IC50 values of 1.3 μM and 0.6 μM, respectively). NZ-97 inhibits the DPP4 pool in lung-resident cells and epithelial lining fluid, elevates IL-6 and IGF-1 levels, and induces the expansion of type 2 alveolar epithelial cells (AEC2). NZ-97 reduces protein content in bronchoalveolar lavage fluid (BALF), ameliorates lung injury and alleviates pulmonary fibrosis. NZ-97 shows tolerability in untreated Mus musculus mice after intratracheal administration, and does not alter the proliferation or differentiation of lung fibroblasts. NZ-97 can be used in studies related to idiopathic pulmonary fibrosis, acute lung injury and emphysema.
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DPP-IV-IN-2
0 ImagesDPP-IV-IN-2 is an inhibitor of both dipeptidyl peptidase IV (DPIV) and DP8/9 with IC50s of 0.1 and 0.95 μM, respectively.
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Glimepiride sulfonamide
0 ImagesGlimepiride sulfonamide acts as both a DPP-IV inhibitor and an α-Amylase inhibitor. It serves as an intermediate for the synthesis of Glimepiride (HY-B0104). Glimepiride sulfonamide stimulates the production and secretion of insulin. It possesses anti-diabetic potential and can be used in diabetes-related research.
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Dutogliptin
0 ImagesSynonyms: PHX-1149 free baseDutogliptin (PHX-1149 free base) is an orally available, potent, and selective dipeptidyl peptidase-4 (DPP4) inhibitor for the treatment of type 2 diabetes mellitus.
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Fotagliptin benzoate
0 ImagesSynonyms: SAL067Fotagliptin benzoate is a Dipeptidyl Peptidase IV (DPP-4) inhibitor (IC50=2.27 nM). Fotagliptin benzoate displays great security in rat and dog. Fotagliptin benzoate can be used for Type 2 diabetes mellitus research.
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Sheng Gelieting
0 ImagesSynonyms: CGT-8012Sheng 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.
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Sitagliptin fenilalanil
0 ImagesSitagliptin fenilalanil is a dipeptidyl aminopeptidase 4 (DPP-4) inhibitor.
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TS-021 free base
0 ImagesSynonyms: DPP-IV-IN-1DPP-IV-IN-1 is a potent inhibitor of dipeptidyl peptidase IV (DPP-IV), a highly specific serine protease, with an IC50 of 4.6 nM.
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AGFAGDDAPR
0 ImagesCat. No.: HY-P60234ACAS No.: 330204-04-1AGFAGDDAPR 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.
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UAMC00039 dihydrochloride
0 ImagesUAMC00039 dihydrochloride is a potent, reversible and competitive dipeptidyl peptidase II inhibitor with an IC50 of 0.48 nM.
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Propyl-GSK-2793660 hydrochloride
0 ImagesPropyl-GSK-2793660 hydrochloride (compound 1) is a irreversible and covalent DPP1 inhibitor. Propyl-GSK-2793660 hydrochloride can be used for the study of bronchiectasis.
