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. 상품명 효과 Purity Chemical Structure
  • HY-176001
    DPP8/9-IN-1
    		Inhibitor
    DPP8/9-IN-1 (Compound 16) is a selective covalent inhibitor of dipeptidyl peptidases 8 and 9 (DPP8/9) with IC50 values of 14 and 298 nM, respectively. DPP8/9-IN-1 binds irreversibly to the active site serine (S730 in DPP9) via a phosphonate warhead and blocks substrate binding to inhibit DPP8/9-mediated protein processing. DPP8/9-IN-1 is promising for research of cancers and inflammatory diseases.
    DPP8/9-IN-1
  • 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
  • HY-120631A
    BMS-538305 hydrochloride
    		Inhibitor
    BMS-538305 hydrochloride is a potent and selective inhibitor of dipeptidyl peptidase IV (DPP-IV), exhibiting strong biological activity by forming a reversible covalent complex with the enzyme. BMS-538305 hydrochloride demonstrates its mechanism of action through the covalent attachment between the nitrile carbon of the inhibitor and the enzyme residue S630, as unveiled by the X-ray crystal structure analysis.
    BMS-538305 hydrochloride
  • HY-123171
    ASP8497
    		Inhibitor
    ASP8497 is a competitive dipeptidyl peptidase IV (DPP-IV) inhibitor that reduces blood glucose levels and increases plasma active GLP-1 and insulin levels without causing hypoglycemia in fasted normal mice. ASP8497 can be utilized for antihyperglycemic research.
    ASP8497
  • HY-159491
    DPP-4-IN-11
    		Inhibitor
    DPP-4-IN-11 (compound 10) is an orally active DPP-4 inhibitor (IC50=2.75 μM) with anti-type 2 diabetes activity. DPP-4-IN-11 exerts its glucose-lowering effect by inhibiting the activities of α-glucosidase (IC50=3.02 μM) and α-amylase (IC50=3.3 μM).
    DPP-4-IN-11
  • HY-P4658
    H-Val-Ala-pNA
    H-Val-Ala-pNA is a substrate for the dipeptide aminopeptidase (DPAPase) of Streptococcus bovis. H-Val-Ala-pNA can be used to measure the activity of the protease.
    H-Val-Ala-pNA
  • HY-151384
    DPP-4-IN-2
    		Inhibitor
    DPP-4-IN-2 (compound b2) is a potent DPP-4 (dipeptidyl peptidase 4) inhibitor, with an IC50of 79 nM. DPP-4-IN-2 is a structurally analogs of Alogliptin (HY-A0023A). DPP-4-IN-2 can be used for diabetes research.
    DPP-4-IN-2
  • HY-10289
    Carmegliptin
    		Inhibitor
    Carmegliptin (RO-4876904) is an orally active and potent DPP IV inhibitor with a human DPP IV IC50 of 6.8 nM. Carmegliptin binds to the S1 pocket of DPP IV, blocks the degradation of GLP 1, potentiates endogenous GLP 1, increases plasma insulin levels, alleviates hyperglycemia, improves glucose tolerance. Carmegliptin acts as a substrate for human P glycoprotein without inhibiting the transporter, shows low in vitro cell permeability. Carmegliptin can be used for the research of type 2 diabetes, non insulin dependent diabetes mellitus.
    Carmegliptin
  • HY-174380
    DPP-1-IN-1
    		Inhibitor
    DPP-1-IN-1 (Compound 14) is an orally active inhibitor of Cathepsin C (also known as Dipeptidyl peptidase I) with an IC50 of 5.31 nM. DPP-1-IN-1 can inhibit the activity of Cathepsin C downstream Neutrophil elastase in neutrophils. DPP-1-IN-1 can be used in the research of inflammatory diseases.
    DPP-1-IN-1
  • HY-146469
    DPP-4/GPR119 modulator 2
    		Inhibitor
    DPP-4/GPR119 modulator 2 (Compound 20i) is a dipeptidyl peptidase IV (DPP-IV) inhibitor and GPR119 agonist with an IC50 of 0.22 μM for DPP-IV and an EC50 of 0.95 μM for GPR119. DPP-4/GPR119 modulator 2 can be used for diabetes research. DPP-4/GPR119 modulator 2 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 2
  • HY-B0422R
    Nateglinide (Standard)
    		Inhibitor
    Nateglinide (Standard) is the analytical standard of Nateglinide. This product is intended for research and analytical applications. Nateglinide, a D-phenylalanine derivative, is an orally active and short-acting insulinotropic agent and a DPP IV inhibitor. Nateglinide inhibits ATP-sensitive K+ channels in pancreatic β-cells. Nateglinide is used for the treatment of type 2 (non-insulin-dependent) diabetes mellitus.
    Nateglinide (Standard)
  • HY-14292
    NVP-DPP728
    		Inhibitor
    NVP-DPP728 is a potent, reversible and nitrile-dependent dipeptidyl peptidase IV (DPP-IV) inhibitor. NVP-DPP728 can inhibit human DPP-IV amidolytic activity with a Ki of 11 nM. NVP-DPP728 inhibits degradation of glucagon-like peptide-1 (GLP-1) and thereby potentiates insulin release in response to glucose intake. NVP-DPP728 can be used for researching diabetes.
    NVP-DPP728
  • HY-182300
    FE 999011
    		Inhibitor
    FE 999011 is an orally active dipeptidyl peptidase IV (DPP-IV) inhibitor with IC50 values of 7 nM and 3 nM against human and rat sources, respectively. FE 999011 acts as a glucose tolerance-improving agent and a GLP-1 receptor activator, which reduces blood glucose fluctuation, promotes GLP-1 release and decreases the insulin-glucose ratio. FE 999011 regulates lipid metabolism, delays the onset of diabetes, stabilizes food and water intake, reduces hypertriglyceridemia, prevents the elevation of free fatty acids, and delays the progression of impaired glucose tolerance to disease. FE 999011 can be used in relevant studies of type 2 diabetes.
    FE 999011
  • HY-15408S
    Trelagliptin-13C,d3
    		Inhibitor
    Trelagliptin-13C,d3 is a deuterated labeled Trelagliptin. 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-<sup>13</sup>C,d<sub>3</sub>
  • HY-P4559
    H-Pro-Met-OH
    		Control
    H-Pro-Met-OH is a dipeptide containing proline and methionine. H-Pro-Met-OH also serves as a substrate for prolinase and prolyl dipeptidase.
    H-Pro-Met-OH
  • HY-P991050
    Procizumab
    		Inhibitor 99%
    Procizumab (AK-1967) is a humanized IgG1 antibody that targets dipeptidyl peptidase 3 (DPP3). Procizumab has the potential for the study of sepsis. The isotype control for Procizumab can refer to Human IgG1 kappa, Isotype Control (HY-P99001).
    Procizumab
  • HY-170657
    DPP-4-IN-14
    		Inhibitor
    DPP-4-IN-14 (compound 30) is a DPP-4 inhibitor, with an IC50 of 12.82 nM.
    DPP-4-IN-14
  • HY-W741755S1
    5-Hydroxy saxagliptin-13C,d2-2 hydrochloride
    		Inhibitor
    5-Hydroxy saxagliptin-13C,d2-2 hydrochloride is the 13C- and deuterium labeled 5-Hydroxy saxagliptin hydrochloride. 5-Hydroxy saxagliptin hydrochloride is an active metabolite of Saxagliptin (HY-10285) and a potent and selective DPP-4 inhibitor. 5-Hydroxy saxagliptin hydrochloride has Ki values of 2.6 nM and 2.9 nM for humans and cynomolgus monkeys, respectively. 5-Hydroxy saxagliptin hydrochloride can be used in the research of type 2 diabetes mellitus.
    5-Hydroxy saxagliptin-<sup>13</sup>C,d<sub>2</sub>-2 hydrochloride
  • HY-122188
    TAK-100
    		Inhibitor
    TAK-100 is a selective and orally active dipeptidyl peptidase IV (DPP-4) inhibitor with an IC50 of 5.3 nM. TAK-100 hass little or no inhibitory effects on other dipeptidyl peptidase members. TAK-100 can be used for the study of diabetes.
    TAK-100
Cat. No. 상품명 / Synonyms Species Source
Cat. No. 상품명 / Synonyms Application Reactivity
Dipeptidyl Peptidase Isoform Comparison

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