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-N8599
    Cichoriin
    		Inhibitor 99.9%
    Cichoriin 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.
    Cichoriin
  • HY-111174A
    Diprotin A TFA
    		Inhibitor 99.62%
    Diprotin A TFA (Ile-Pro-Ile TFA) is an inhibitor of dipeptidyl peptidase IV (DPP-IV).
    Diprotin A TFA
  • HY-14892B
    Gemigliptin tartrate hydrate
    		Inhibitor 99.83%
    Gemigliptin (LC15-0444 ) tartrate hydrate is a selective, reversible and competitive dipeptidyl peptidase-4 (DPP-4) inhibitor, with an IC50 of 10.3 nM for human recombinant DPP-4. Gemigliptin tartrate hydrate exhibits potent anti-glycation properties. Gemigliptin tartrate hydrate can be used for the research of advanced glycation end products (AGE)-related diabetic complications.
    Gemigliptin tartrate hydrate
  • HY-10286
    Dutogliptin
    		Inhibitor 99.21%
    Dutogliptin (PHX-1149 free base) is an orally available, potent, and selective dipeptidyl peptidase-4 (DPP4) inhibitor for the treatment of type 2 diabetes mellitus.
    Dutogliptin
  • HY-13749S1
    Sitagliptin-d4 hydrochloride
    		99.36%
    Sitagliptin-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.
    Sitagliptin-d<sub>4</sub> hydrochloride
  • HY-147401
    Sitagliptin fenilalanil
    		Inhibitor 99.57%
    Sitagliptin fenilalanil is a dipeptidyl aminopeptidase 4 (DPP-4) inhibitor.
    Sitagliptin fenilalanil
  • HY-U00346
    TS-021 free base
    		Inhibitor 98.84%
    DPP-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.
    TS-021 free base
  • HY-10285A
    Saxagliptin hydrate
    		Inhibitor ≥99.0%
    Saxagliptin 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.
    Saxagliptin hydrate
  • HY-158315
    NZ-97
    		Inhibitor 99.43%
    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-P991551
    YS110
    		Inhibitor 99.14%
    YS110 is a humanized anti-CD26 (DPP4) IgG1 monoclonal antibody. YS110 induces CD26 nuclear translocation through the caveolin pathway. YS110 inhibits the proliferation of tumor cell by delaying G2/M cell cycle transition. YS110 inhibits the infection of Middle East respiratory syndrome coronavirus (MERS CoV) by blocking the binding of MERS CoV S1 to CD26. YS110 can be used for researches on cancer or infection such as Malignant Mesothelioma and MERS.
    YS110
  • HY-101769
    UAMC00039 dihydrochloride
    		Inhibitor 99.49%
    UAMC00039 dihydrochloride is a potent, reversible and competitive dipeptidyl peptidase II inhibitor with an IC50 of 0.48 nM.
    UAMC00039 dihydrochloride
  • HY-111173
    Diprotin B
    		Activator 99.60%
    Diprotin 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.
    Diprotin B
  • HY-P4558A
    H-Pro-Lys-OH TFA
    		Substrate
    H-Pro-Lys-OH TFA is a dipeptide containing proline and lysine, which can serve as a substrate for iminodipeptidase (prolinase). H-Pro-Lys-OH TFA can also be used for the synthesis of polypeptides.
    H-Pro-Lys-OH TFA
  • HY-148190
    Sheng Gelieting
    		Inhibitor 98.29%
    Sheng 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.
    Sheng Gelieting
  • HY-N7653
    Azaleatin
    		Inhibitor 98.80%
    Azaleatin is an O-methylated flavonol isolated from Rhododendron species. Azaleatin is a dipeptidyl peptidase-IV inhibitor. Azaleatin can be used for the research of type-2 diabetes and obesity.
    Azaleatin
  • HY-120709
    Propyl-GSK-2793660 hydrochloride
    		Inhibitor 98.71%
    Propyl-GSK-2793660 hydrochloride (compound 1) is a irreversible and covalent DPP1 inhibitor. Propyl-GSK-2793660 hydrochloride can be used for the study of bronchiectasis.
    Propyl-GSK-2793660 hydrochloride
  • HY-131250
    N-Boc-Sitagliptin
    		98.87%
    N-Boc-Sitagliptin is an intermediate in the synthesis of the dipeptidyl peptidase 4 (DPP-4) inhibitor Sitagliptin (HY-13749).
    N-Boc-Sitagliptin
  • HY-A0023R
    Alogliptin Benzoate (Standard)
    		Inhibitor
    Alogliptin (Benzoate) (Standard) is the analytical standard of Alogliptin (Benzoate). This product is intended for research and analytical applications. 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 (Standard)
  • 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.
    Gemigliptin
  • HY-14291A
    Vildagliptin dihydrate
    		Inhibitor
    Vildagliptin dihydrate (LAF237 dihydrate) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin dihydrate possesses excellent oral bioavailability and potent antihyperglycemic activity.
    Vildagliptin dihydrate
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Dipeptidyl Peptidase Isoform Comparison

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