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-182336
    DeDPP4
    		Inhibitor
    DeDPP4 is a DPP-4 PROTAC degrader. DeDPP4 induces sustained elevation of glucagon-like peptide-1 (GLP-1), enhances glucose tolerance, causes persistent reduction of blood glucose, and achieves long-term blood glucose regulation in animal models of type 2 diabetes. DeDPP4 mediates dose-dependent DPP-4 depletion in cancer cells, and also targets and degrades DPP-4 in the liver and adipose tissues of animal models with type 2 diabetes. DeDPP4 can be used for the research of type 2 diabetes and non-small cell lung cancer.
    DeDPP4
  • HY-P4488
    H-Pro-Pro-Gln-OH
    		Inhibitor
    H-Pro-Pro-Gln-OH is a oligopeptide with excellent dipeptidyl peptidase-IV (DPP-IV) inhibitory activity.
    H-Pro-Pro-Gln-OH
  • HY-10284S1
    Linagliptin-13C,d3
    		Inhibitor
    Linagliptin-13C,d3 is the 13C- and deuterium labeled Linagliptin. Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM. Linagliptin-13C,d3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Linagliptin-<sup>13</sup>C,d<sub>3</sub>
  • 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-10285S
    Saxagliptin-15N,d2 Hydrochloride
    		Inhibitor
    Saxagliptin-15N,d2 Hydrochloride (BMS-477118-15N,d2 Hydrochloride) is the 15N and deuterium labeled isotope of Saxagliptin (HY-10285). 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>15</sup>N,d<sub>2</sub> Hydrochloride
  • HY-W741755A
    5-Hydroxy saxagliptin hydrochloride
    		Inhibitor
    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 hydrochloride
  • HY-160073A
    Florensocatib hydrate
    		Inhibitor
    Florensocatib hydrate is a DPP1 inhibitor (IC50: 1.6 nM). Florensocatib hydrate has good bioavailability and pharmacokinetic characteristics, and can be used for research of inflammatory disease.
    Florensocatib hydrate
  • HY-182374
    AX8819
    		Inhibitor
    AX8819 is a selective dipeptidyl peptidase II (DPP II) inhibitor with an IC50 of 0.88 nM. AX8819 induces caspase-dependent apoptosis. AX8819 exhibits low non-specific toxicity toward proliferating T cells. AX8819 can be used for the research of B cell chronic lymphocytic leukemia.
    AX8819
  • HY-N17777
    Cyclocarin A
    		Inhibitor
    Cyclocarin A is a triterpenoid compound that can be isolated from the leaves of Cyclocarya paliurus. Cyclocarin A shows only weak inhibitory activity against α-glucosidase, lipase, DPP-IV, aldose reductase, and human cancer cell lines (IC50>10 μM).
    Cyclocarin A
  • HY-13749S2
    Sitagliptin-d4
    		Inhibitor
    Sitagliptin-d4 (MK-0431-d4) 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>4</sub>
  • 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-16656
    BMS-767778
    		Inhibitor
    BMS-767778 is an orally active and selective DPP4 inhibitor with Ki values of 0.94 nM, 4.9, 3.2 nM for DPP4, DPP8 and DPP9 respectively. BMS-767778 exhibits >3,000-fold selectivity over the related enzymes DPP8 and DPP9. BMS-767778 inhibits CYP-3A4 with IC50 of 5.2 μM. BMS-767778 significantly reduces blood glucose levels in high fat fed (HFD) ob/ob mice with safety profile. BMS-767778 can be used for diabetes mellitus research.
    BMS-767778
  • 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-125330
    Denagliptin tosylate
    		Inhibitor
    Denagliptin tosylate is the tosyate salt form of Denagliptin. Denagliptin tosylate is a small molecule dipeptidyl peptidase IV (DPP-4) inhibitor. It can be used in type 2 diabetes research.
    Denagliptin tosylate
  • 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-10287A
    Gosogliptin hydrochloride
    		Inhibitor
    Gosogliptin hydrochloride is the hydrochloride of Gosogliptin (HY-10287). Gosogliptin (PF-00734200) is a potent, orally active, selective, and competitive inhibitor of DPP-IV, the enzyme mainly responsible for the degradation of the incretin peptides GLP-1 and glucose-dependent insulinotropic polypeptide. Gosogliptin demonstrates rapid and reversible inhibition of plasma DPP-4 activity. Gosogliptin stimulates insulin secretion and improves glucose tolerance.
    Gosogliptin hydrochloride
  • 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Dipeptidyl Peptidase Isoform Comparison

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