1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. Dipeptidyl Peptidase

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-151871
    ICeD-2
    Inhibitor
    ICeD-2 is a inducer of cell death, can induce HIV-1 infected cell kill. ICeD-2-mediated HIV-1 infected cell kill is dependent on HIV-1 protease activity. ICeD-2 potently blocks hydrolysis of Gly-Pro-AMC by dipeptidyl peptidase DPP8 and DPP9. ICeD-2 shows strong stabilization of DPP9 in PBMCs.
    ICeD-2
  • HY-B0422S
    Nateglinide-d5
    Inhibitor 98.0%
    Nateglinide-d5 is a deuterium labeled Nateglinide. 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[1][2].
    Nateglinide-d<sub>5</sub>
  • HY-101605
    Prodipine hydrochloride
    Inhibitor 99.84%
    Prodipine, a diphenyl-phosphonate derivative. The IC50s of Prodipine for purified and plasma Dipeptidyl peptidase IV (DPP IV) from the rabbit are 4.5 μM and 30 μM, respectively.
    Prodipine hydrochloride
  • HY-P10809
    VAMP
    Inhibitor 98.13%
    VAMP, a tetrapeptide, is a competitive dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 1.00 μM and a Kd of 6.89 μM. VAMP effectively targets the DPP-IV-GLP-1 axis and can be used for the study of type 2 diabetes.
    VAMP
  • HY-P4558
    H-Pro-Lys-OH
    Control 99.69%
    H-Pro-Lys-OH is a dipeptide containing proline and lysine, which can serve as a substrate for iminodipeptidase (prolinase). H-Pro-Lys-OH can also be used for the synthesis of polypeptides.
    H-Pro-Lys-OH
  • HY-W121887
    Zomepirac acyl-O-β-D-glucuronide
    Inhibitor
    Zomepirac acyl-O-β-D-glucuronide (Zomepirac glucuronide) is a dipeptidyl peptidase IV Inhibitor. Zomepirac acyl-O-β-D-glucuronide is an unstable and chemically reactive metabolite of Zomepirac (HY-B0890A). Zomepirac acyl-O-β-D-glucuronide forms covalent adducts with cell membrane glycoproteins. Zomepirac acyl-O-β-D-glucuronide can be used for research on immunotoxicity.
    Zomepirac acyl-O-β-D-glucuronide
  • HY-W744745
    Linagliptin methyldimer
    Control
    Linagliptin methyldimer is an impurity of Linagliptin. Linagliptin is a DPP-IV inhibitor, with IC50 of 1 nM.
    Linagliptin methyldimer
  • HY-I0786
    (2S,4R)-Teneligliptin
    Inhibitor
    (2S,4R)-Teneligliptin is a selective inhibitor of dipeptidyl peptidase IV (DPP-4). (2S,4R)-Teneligliptin increases the plasma concentration of active glucagon-like peptide-1 (GLP-1), which promotes insulin secretion in response to elevated blood glucose levels, exerting hypoglycemic activity. (2S,4R)-Teneligliptin is promising for research of type 2 diabetes.
    (2S,4R)-Teneligliptin
  • HY-12733
    AZD5248
    Inhibitor 98.9%
    AZD5248 is a dipeptidyl peptidase 1 (DPP1) inhibitor that can be used for the research of chronic obstructive lung disease.
    AZD5248
  • HY-A0023AS2
    Alogliptin-13C,d3 benzoate
    Inhibitor 98.77%
    Sulfo DBCO-PEG4-Maleimide TEA is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
    Alogliptin-<sup>13</sup>C,d<sub>3</sub> benzoate
  • HY-12528
    DBPR108
    Inhibitor 99.93%
    DBPR108 is a potent, selective, and orally bioavailable dipeptide-derived inhibitor of DPP4 with IC50 of 15 nM; no inhibition on DDP8 and DPP9.
    DBPR108
  • HY-117985
    Evogliptin
    Inhibitor
    Evogliptin (DA-1229) is an orally active DPP4 inhibitor with significant and sustained hypoglycaemic effects in mouse models. Evogliptin also inhibits the production of inflammatory and fibrotic signals in hepatocytes by inducing autophagy. Evogliptin can be used in studies of type 2 diabetes, osteoporosis, renal impairment and chronic liver inflammation.
    Evogliptin
  • HY-112668B
    Retagliptin hydrochloride
    Inhibitor
    Retagliptin (SP2086) hydrochloride is a potent inhibitor of beta-amino acids and dipeptidyl peptidase-4 (DPP-4). Retagliptin (SP2086) hydrochloride inhibits type 2 diabetes and improves glycemic control by prolonging the action of intestinal hormones such as glucagon-like peptide-1 (GLP-1).
    Retagliptin hydrochloride
  • HY-170569
    Cetagliptin
    Inhibitor
    Cetagliptin is an orally active inhibitor for dipeptidyl peptidase 4 (DPP-4) and CYP2D6 (IC50 of 6 µM). Cetagliptin is a substrate for P-glycoprotein. Cetagliptin reduces the GLP-1 degradation, maintains the level of postprandial blood sugar, and can be used in type 2 diabetes mellitus research.
    Cetagliptin
  • HY-117985A
    Evogliptin hydrochloride
    Inhibitor
    Evogliptin hydrochloride (DA-1229 hydrochloride) is an orally available DPP4 inhibitor with significant and durable hypoglycemic effects in mouse models. Evogliptin hydrochloride also inhibits the generation of inflammatory and fibrotic signals in hepatocytes by inducing autophagy. Evogliptin hydrochloride can be used in the research of type 2 diabetes, osteoporosis, renal impairment and chronic liver inflammation.
    Evogliptin hydrochloride
  • HY-10286A
    Dutogliptin tartrate
    Inhibitor
    Dutogliptin tartrate (PHX-1149) is an orally available, potent, and selective dipeptidyl peptidase-4 (DPP4) inhibitor for the treatment of type 2 diabetes mellitus.
    Dutogliptin tartrate
  • HY-14877A
    Anagliptin hydrochloride
    Inhibitor
    Anagliptin (SK-0403) hydrochloride is a highly selective, potent, orally active inhibitor of dipeptidyl peptidase 4 (DPP-4), with an IC50 of 3.8 nM, and less selective at DPP-8 and DDP-9 with IC50s of 68 nM and 60 nM, respectively.
    Anagliptin 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-Z1764
    DPP-4-IN-18
    Inhibitor
    DPP-4-IN-18 (Sitagliptin impurity 3) (Compound 4) impurity 3 is a potent, selective and orally active DPP-4 inhibitor with an IC50 of 27 nM. DPP-4-IN-18 can effectively prevent DPP-4 from degrading glucagon-like peptide 1 (GLP-1), thereby increasing the level of active GLP-1. DPP-4-IN-18 can be used for the research of type 2 diabetes.
    DPP-4-IN-18
  • 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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