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-14806S1
    Teneligliptin-d4
    		Inhibitor
    Teneligliptin-d4 is deuterium labeled Teneligliptin. Teneligliptin (MP-513) is a potent, orally available, competitive, and long-lasting DPP-4 inhibitor. Teneligliptin competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM.
    Teneligliptin-d<sub>4</sub>
  • HY-N9725
    16-Hydroxycleroda-3,13-dien-15,16-olide
    		Inhibitor
    16-Hydroxycleroda-3,13-dien-15,16-olide (16ξ-Hydroxycleroda-3,13-dien-15,16-olide; HCD), a clerodane diterpene, is a potent serine protease dipeptidyl peptidase 4 (DPP-4) inhibitor. 16-Hydroxycleroda-3,13-dien-15,16-olide down-regulates LPS-induced ERK phosphorylation in myocyte but blocks GLP-1 induced PKA expression. 16-Hydroxycleroda-3,13-dien-15,16-olide exhibits hypolipidemic, hepatoprotective, hypoglycemic efficacy.
    16-Hydroxycleroda-3,13-dien-15,16-olide
  • HY-163335
    MPO-IN-7
    		Inhibitor
    MPO-IN-7 (compound MDC) is a myeloperoxidase inhibitor with the IC50 values of 41 μM, 25 μM and 4.5 μM towards α-Glucosidase, dipeptidyl peptidase-4 and myeloperoxidase, respectively. MPO-IN-7 shows antioxidant and anti-inflammatory activity in vitro.
    MPO-IN-7
  • HY-10284S3
    Linagliptin-d3-1
    		Inhibitor
    Linagliptin-d3-1 (BI 1356-d3-1) is the deuterium labeled Linagliptin (HY-10284). Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM.
    Linagliptin-d<sub>3</sub>-1
  • HY-176000
    Sulphostin
    		Inhibitor
    Sulphostin is a covalent inhibitor of dipeptidyl peptidase 4 (DPP4), dipeptidyl peptidase 9 (DPP9), and dipeptidyl peptidase 8 (DPP8) with IC50 values of 79, 1392, 6930 nM, respectively. Sulphostin causes phosphosulfamate modification, irreversibly inhibits the enzyme activity. Sulphostin can be used for inflammation and cancer study.
    Sulphostin
  • HY-129736
    P32/98 hemifumarate
    		Inhibitor
    P32/98 hemifumarateis a potent inhibitor of dipeptidyl peptidase IV with a Ki value of 130 nM. P32/98 hemifumarate improves glucose tolerance, insulin sensitivity and β-cell responsiveness in fatty Zucker rat model.
    P32/98 hemifumarate
  • HY-172529
    DPP9-IN-1
    		Inhibitor
    DPP9-IN-1 (Compound 42) is a dipeptidyl peptidase 9 (DPP9) inhibitor with IC50 of 3 nM for DPP9 and 0.6 μM for DPP8. DPP9-IN-1 induces concentration-dependent LDH release in THP-1 cells.
    DPP9-IN-1
  • HY-129736A
    P32/98
    		Inhibitor
    P32/98 a potent inhibitor of dipeptidyl peptidase IV with a Ki value of 130 nM. P32/98 improves glucose tolerance, insulin sensitivity and β-cell responsiveness in fatty Zucker rat model.
    P32/98
  • HY-P6177
    SGP8
    		Inhibitor
    SGP8 (IAVPGEVA) is an octapeptide produced by hydrolysis of soybean 11S globulin, which has the effects of regulating lipid metabolism, inflammation and fibrosis. SGP8 (IAVPGEVA) exhibits inhibitory activity against DPP4 and inhibits the JNK-c-Jun signaling pathway, and has the ability to inhibit non-alcoholic steatohepatitis (NASH).
    SGP8
  • HY-169110
    DPP-4-IN-12
    		Inhibitor
    DPP-4-IN-12 (compound 46) is a potent DPP-4 inhibitor with IC50 value of 2 nM. DPP-4-IN-12 can be used in the study of type 2 diabetes.
    DPP-4-IN-12
  • HY-P4345
    Pro-Arg-AMC
    		Substrate
    Pro-Arg-AMC is a peptide substrate of DPAP1.
    Pro-Arg-AMC
  • HY-155027
    DPP-4-IN-8
    		Inhibitor
    DPP-4-IN-8 (compound 27) is a potent and selective DPP4 (dipeptidyl peptidase 4) inhibitor, with a Ki of 0.96 μM. DPP-4-IN-8 blocks the dipeptidase activity of DPP4 in both Caco-2 and HepG-2 cells. DPP-4-IN-8 also dose-dependently suppresses the expression levels of the chemokines tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6), and interleukin-1β (IL-1β).
    DPP-4-IN-8
  • HY-P4558
    H-Pro-Lys-OH
    		Control
    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-13749R
    Sitagliptin (Standard)
    		Inhibitor
    Sitagliptin (Standard) is the analytical standard of Sitagliptin (HY-13749). This product is intended for research and analytical applications. 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 (Standard)
  • HY-15408AR
    Trelagliptin succinate (Standard)
    		Inhibitor
    Trelagliptin (succinate) (Standard) is the analytical standard of Trelagliptin (succinate). This product is intended for research and analytical applications. Trelagliptin (SYR-472) succinate 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 succinate (Standard)
  • HY-13749CR
    (S)-Sitagliptin phosphate (Standard)
    		Inhibitor
    (S)-Sitagliptin (phosphate) (Standard) is the analytical standard of (S)-Sitagliptin (phosphate). This product is intended for research and analytical applications. (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 (Standard)
  • HY-14806R
    Teneligliptin (Standard)
    		Inhibitor
    Teneligliptin (Standard) is the analytical standard of Teneligliptin. This product is intended for research and analytical applications. Teneligliptin (MP-513) is a potent, orally available, competitive, and long-lasting DPP-4 inhibitor. Teneligliptin competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM.
    Teneligliptin (Standard)
  • HY-N8134
    2-Methoxy-5-acetoxy-fruranogermacr-1(10)-en-6-one
    		Inhibitor
    2-Methoxy-5-acetoxy-fruranogermacr-1(10)-en-6-one is a natural product found in the leaves and stem bark of M. glabra. 2-Methoxy-5-acetoxy-fruranogermacr-1(10)-en-6-one displays binding affinities with dipeptidyl peptidase-4 (DPP-4) and α-Amylase. 2-Methoxy-5-acetoxy-fruranogermacr-1(10)-en-6-one has potential antidiabetic activities.
    2-Methoxy-5-acetoxy-fruranogermacr-1(10)-en-6-one
  • HY-170800
    DPP-4-IN-15
    		Inhibitor
    DPP-4-IN-15 (Compound 22) is a non-competitive inhibitor of dipeptidyl peptidase-4 (DPP-4) with an IC50 of 8.24 μM.
    DPP-4-IN-15
  • HY-10285AR
    Saxagliptin hydrate (Standard)
    		Inhibitor
    Saxagliptin (hydrate) (Standard) is the analytical standard of Saxagliptin (hydrate). This product is intended for research and analytical applications. 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 (Standard)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Dipeptidyl Peptidase Isoform Comparison

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