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-147401A
    Sitagliptin fenilalanil hydrochloride
    		Inhibitor 98.94%
    Sitagliptin fenilalanil hydrochloride is a dipeptidyl aminopeptidase 4 (DPP-4) inhibitor.
    Sitagliptin fenilalanil hydrochloride
  • HY-N10360
    Ellipyrone A
    		Inhibitor
    Ellipyrone A, a γ-pyrone enclosed macrocyclic poyketide, shows inhibition potential against dipeptidyl peptidase-4 (IC50=0.35 mM). Ellipyrone A also has anti-carbolytic property against α-glucosidase (IC50=0.74 mM) and α-amylase (IC50=0.59 mM).
    Ellipyrone A
  • HY-13749C
    (S)-Sitagliptin phosphate
    		Inhibitor
    (S)-Sitagliptin phosphate is the less active S-enantiomer of Sitagliptin phosphate. Sitagliptin phosphate (MK-0431 phosphate) is a potent inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts.
    (S)-Sitagliptin phosphate
  • HY-14293
    NVP-DPP728 dihydrochloride
    		Inhibitor
    NVP-DPP728 dihydrochloride is a potent, selective and orally active dipeptidyl peptidase IV (DPP-IV) inhibitor with a Ki of 11 nM. NVP-DPP728 dihydrochloride can be used for the research of diabetes mellitus.
    NVP-DPP728 dihydrochloride
  • HY-163332
    MPO-IN-6
    		Inhibitor
    MPO-IN-6 (compound ADC) is an electrophile with good antioxidant and anti-inflammatory properties. MPO-IN-6 is a myeloperoxidase (MPO), dipeptidyl peptidase-4 (DPP-4), and α-glucosidase (α-GD) inhibitor with IC50s of 10 μM, 31.02 μM, and 46.05 μM, respectively. MPO-IN-6 is a potential cardiovascular preventive agent.
    MPO-IN-6
  • HY-N10362
    Ellipyrone B
    		Inhibitor
    Ellipyrone B, an antihyperglycemic γ-pyrone enclosed macrocyclic polyketide, shows inhibition potential against dipeptidyl peptidase-4 (IC50=0.48 mM).
    Ellipyrone B
  • HY-156846
    O-Benzoylhydroxylamine
    		Inhibitor
    O-Benzoyl hydroxylamine is a DPP-IV inhibitor with anti-diabetic effects (WO2006034435A2).
    O-Benzoylhydroxylamine
  • HY-155961
    Antidiabetic agent 2
    		Inhibitor
    Antidiabetic agent 2 (Compound 56) is a glucose-uptake promoter. Antidiabetic agent 2 inhibits DPP-4, PTP-1B, α-amylase, and α-glucosidase with IC50s of 0.036, 0.042, 0.241, 0.185 μM. Antidiabetic agent 2 decreases blood glucose levels.
    Antidiabetic agent 2
  • HY-146468
    DPP-4/GPR119 modulator 1
    		Inhibitor
    DPP-4/GPR119 modulator 1 (Compound 22) is an orally active dipeptidyl peptidase IV (DPP-IV) inhibitor and GPR119 agonist. DPP-4/GPR119 modulator 1 shows blood glucose-lowering effect and moderate inhibition on hERG channel with an IC50 of 4.9 μM. DPP-4/GPR119 modulator 1 can be used for diabetes research. DPP-4/GPR119 modulator 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    DPP-4/GPR119 modulator 1
  • 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-146455
    DPP-4-IN-3
    		Inhibitor
    DPP-4-IN-3 (Compound 5a) is a potent dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 0.75 nM. DPP-4-IN-3 shows excellent antioxidant and insulinotropic activity.
    DPP-4-IN-3
  • HY-D2327
    DPP-8/9 probe-1
    		Inhibitor
    DPP-8/9 probe-1 (compound 20) is a fluorescent probe targeting Dipeptidyl Peptidase DPP8/9, which can be selectively labeled and visualized in vitro by fluorescence microscopy Active DPP8/9. DPP-8/9 probe-1 contains a nitrobenzoxadiazole (NBD) tag and has high affinity and selectivity for DPP8/9 over related S9 family members (IC50 of 210 nM and 15 nM, respectively).
    DPP-8/9 probe-1
  • HY-160073A
    DPP1-IN-1 hydrate
    		Inhibitor
    DPP1-IN-1 hydrate is a DPP1 inhibitor (IC50: 1.6 nM). DPP1-IN-1 hydrate has good bioavailability and pharmacokinetic characteristics, and can be used for research of inflammatory disease.
    DPP1-IN-1 hydrate
  • HY-111150
    AMG-222
    		Inhibitor
    AMG-222 is a dipeptidyl peptidase IV (DPP-IV) inhibitor that exerts its inhibitory effect by tightly and reversibly binding to DPPIV. AMG 222 binds to human plasma proteins in a saturable and concentration-dependent manner, with a binding rate of 80.8% at 1 nM, while the binding rate decreases to 29.4% at concentrations above 100 nM. AMG-222 can be used in research related to diabetes.
    AMG-222
  • HY-14291S2
    Vildagliptin-13C5,15N
    		Inhibitor
    Vildagliptin-13C5,15N (LAF237-13C5,15N; NVP-LAF 237-13C5,15N) is a 13C- and 15N-labeled Vildagliptin (HY-14291). 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-<sup>13</sup>C<sub>5</sub>,<sup>15</sup>N
  • HY-151383
    DPP-4-IN-1
    		Inhibitor
    DPP-4-IN-1 (compound d1) is a potent DPP-4 (dipeptidyl peptidase 4) inhibitor, with an IC50of 49 nM. DPP-4-IN-1 is a structurally analogs of Alogliptin (HY-A0023A). DPP-4-IN-1 can be used for diabetes research.
    DPP-4-IN-1
  • HY-157390
    DPP-4-IN-9
    		Inhibitor
    DPP-4-IN-9 (compound 6l) is a potent inhibitor of dipeptidyl peptidase DPP-4 (IC50: 8.22 nM). DPP-4-IN-9 has antihyperglycemic activity.
    DPP-4-IN-9
  • HY-162513
    DPP-4-IN-10
    		Inhibitor
    DPP-4-IN-10 (compound 1) is a DPP-4 inhibitor. DPP-4-IN-10 is orally active. DPP-4-IN-10 blocks the degradation of GLP-1 and GIP, which may improve glycemic control in type 2 diabetes (T2MD).
    DPP-4-IN-10
  • HY-151578
    DPP IV/hCA II-IN-1
    		Inhibitor
    DPP IV/hCA II-IN-1 is a potent and selective dipeptidyl peptidase IV (DPP IV) and carbonic anhydrase (CA) inhibitor with an IC50 value of 0.049 μM for DPP IV and with Ki values of 0.0361, 0.0428, 0.0941, 0.1328, 0.2615, and 3.034 μM for CA II, CA VB, CA VA, CA IX, CA I, and CA IV, respectively.
    DPP IV/hCA II-IN-1
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Dipeptidyl Peptidase Isoform Comparison

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