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-10288
    Melogliptin
    		Inhibitor
    Melogliptin is a DPP-4 inhibitor. Melogliptin can be used in the research of type 2 diabetes.
    Melogliptin
  • HY-179473
    MK-0626
    		Inhibitor
    MK-0626 is a selective, orally active DPP-4 inhibitor with an IC50 of 6.3 nM. MK-0626 increases endothelial nitric oxide synthetase expression. MK-0626 improves neovascularization, attenuates hepatic steatosis, attenuates pancreatic islet injury. MK-0626 can be used in the research of diabetes and non-alcoholic fatty liver disease.
    MK-0626
  • 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-N17532
    (Rac)-Regaloside D
    (Rac)-Regaloside D is a phenylpropanoid. (Rac)-Regaloside D can be found in the scaly bulbs of Lilium longiflorum. (Rac)-Regaloside D does not exhibit dipeptidyl peptidase IV (DPP-IV) inhibitory activity in vitro.
    (Rac)-Regaloside D
  • HY-10289A
    Carmegliptin hydrochloride
    		Inhibitor
    Carmegliptin hydrochloride (RO-4876904 hydrochloride) is an orally active and potent DPP‑IV inhibitor with a human DPP‑IV IC50 of 6.8 nM. Carmegliptin hydrochloride 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 hydrochloride acts as a substrate for human P‑glycoprotein without inhibiting the transporter, shows low in vitro cell permeability. Carmegliptin hydrochloride can be used for the research of type 2 diabetes, non‑insulin‑dependent diabetes mellitus.
    Carmegliptin hydrochloride
  • 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-172242
    Verducatib
    		Inhibitor 98.94%
    Verducatib (BI 1291583) is an orally active inhibitor of cathepsin C (also known as DPP1). Verducatib restores the protease-inhibitor balance by inhibiting the activation of neutrophil serine proteases, thereby alleviating pulmonary inflammation and regulating infection responses. Verducatib significantly reduces the risk (including severe exacerbations) and frequency of acute exacerbations in bronchiectasis (BE). Verducatib also improves lung function and quality of life, and shortens the duration of antibiotic use. The overall incidence of adverse events of Verducatib is comparable to that of placebo, with only slightly more mild-to-moderate cutaneous adverse events observed in the high-dose group, demonstrating promising clinical application potential.
    Verducatib
  • 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-13749E
    Sitagliptin hydrochloride
    		Inhibitor
    Sitagliptin (MK-0431) hydrochloride is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin hydrochloride 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 hydrochloride 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 hydrochloride shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin hydrochloride can be used for the study of 1-type and 2-type diabetes.
    Sitagliptin hydrochloride
  • 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-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)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Dipeptidyl Peptidase Isoform Comparison

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