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-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-180527
    SGLT2-IN-5
    		Inhibitor
    SGLT2-IN-5 (Compound 99) is an orally active SGLT2 inhibitor with IC₅₀ values for SGLT2, SGLT1, and DPP4 of 0.8, 23, and 58 nM respectively. SGLT2-IN-5 controls blood sugar levels in diabetic rat models and increases the levels of active GLP-1. SGLT2-IN-5 can be used for the study of type 2 diabetes.
    SGLT2-IN-5
  • 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 99.70%
    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)
  • HY-175590
    DPP-4-IN-17
    		Inhibitor
    DPP-4-IN-17 is an orally active and selective dipeptidyl peptidase-4 (DPP-4) inhibitor with an IC50 value of 0.12 nM. DPP-4-IN-17 increases the enzyme's Km value (75.73 μM vs. 27.18 μM of substrate alone) and reduces catalytic efficiency. DPP-4-IN-17 reduces blood glucose levels and reverses weight loss in Streptozotocin (STZ) (HY-13753)/Nicotinamide (NA) (HY-B0150)-induced diabetic rats. DPP-4-IN-17 can be used for the study of type 2 diabetes mellitus (T2DM).
    DPP-4-IN-17
  • HY-14291R
    Vildagliptin (Standard)
    		Inhibitor
    Vildagliptin (Standard) is the analytical standard of Vildagliptin. This product is intended for research and analytical applications. 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 (Standard)
  • HY-13749S3
    Sitagliptin-d6
    		Inhibitor
    Sitagliptin-d6 (MK-0431-d6) 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>6</sub>
  • HY-10285S1
    (rel)-Saxagliptin-13C,d2 TFA
    		Inhibitor
    (rel)-Saxagliptin-13C,d2 ((rel)-BMS-477118-13C,d2) TFA is 13C-labeled Saxagliptin (HY-10285).
    (rel)-Saxagliptin-<sup>13</sup>C,d<sub>2</sub> TFA
  • HY-108319R
    DPP-IV-IN-2 (Standard)
    		Inhibitor
    DPP-IV-IN-2 (Standard) is the analytical standard of DPP-IV-IN-2 (HY-108319). This product is intended for research and analytical applications. DPP-IV-IN-2 is an inhibitor of both dipeptidyl peptidase IV (DPIV) and DP8/9 with IC50s of 0.1 and 0.95 μM, respectively.
    DPP-IV-IN-2 (Standard)
  • HY-132489S
    (Rac)-Sitagliptin-d4
    		Inhibitor
    (Rac)-Sitagliptin-d4 ((Rac)-MK-0431-d4) is the deuterium labeled (Rac)-Sitagliptin. (Rac)-Sitagliptin is an isoform of Sitagliptin (HY-13749), which is a potent and orally active inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts.
    (Rac)-Sitagliptin-d<sub>4</sub>
  • HY-N14989A
    Fluostatin A sodium
    		Inhibitor
    Fluostatin A sodium is a dipeptidyl peptidaseIII inhibitor with an IC50 of 0.44 μg/mL. Fluostatin A can be extracted from Streptomyces sp. TA-3391.
    Fluostatin A sodium
  • HY-N14989
    Fluostatin A
    		Inhibitor
    Fluostatin A inhibits the ability of DPP-III, and with arginyl-arginine-2-naphthalene formamide as the substrate, the IC50 is 0.44 μg/mL.
    Fluostatin A
  • HY-180528
    SGLT2-IN-6
    		Inhibitor
    SGLT2-IN-6 (Compound 101) is an orally active SGLT2 inhibitor with IC₅₀ values for SGLT2, SGLT1, and DPP4 of 0.8, 6.7, and 72 nM respectively. SGLT2-IN-6 controls blood sugar levels in diabetic rat models and increases the levels of active GLP-1. SGLT2-IN-6 can be used for the study of type 2 diabetes.
    SGLT2-IN-6
  • HY-14806S2
    Teneligliptin-d5
    		Inhibitor
    Teneligliptin-d5 (MP-513-d5) is deuterium labeled Teneligliptin. Teneligliptin (MP-513) hydrobromide hydrate is an orally active and selective dipeptidyl peptidase 4 (DPP-4) inhibitor (IC50s: 0.37 and 0.29 nM for the human and rat DPP-4, respectively). Teneligliptin hydrobromide hydrate improves blood glucose levels and can be used in researches related to type 2 diabetes mellitus.
    Teneligliptin-d<sub>5</sub>
  • HY-19859
    AMG-222 tosylate
    AMG-222 (tosylate) is a DPP-IV inhibitor that can be used in the research of type II diabete.
    AMG-222 tosylate
  • HY-151871A
    cis-ICeD-2
    		Inhibitor
    cis-ICeD-2 is the cis isomer of ICeD-2 (HY-151871). ICeD-2 is a cell death inducer that induces cell death in HIV-1-infected cells. ICeD-2-mediated killing of HIV-1-infected cells is dependent on HIV-1 protease activity. ICeD-2 effectively blocks the hydrolysis of Gly-Pro-AMC by the dipeptidyl peptidases DPP8 and DPP9. ICeD-2 demonstrates strong stability against DPP9 in PBMCs..
    cis-ICeD-2
  • HY-132489S1
    (Rac)-Sitagliptin-d4-1 hydrochloride
    		Inhibitor
    (Rac)-Sitagliptin-d4-1 hydrochloride ((Rac)-MK-0431-d4-1 hydrochloride) is the deuterium labeled (Rac)-Sitagliptin-1 hydrochloride. (Rac)-Sitagliptin is an isoform of Sitagliptin (HY-13749), which is a potent and orally active inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts.
    (Rac)-Sitagliptin-d<sub>4</sub>-1 hydrochloride
  • HY-N15181
    Fluostatin B
    		Inhibitor
    Fluostatin B is a dipeptidyl peptidase 3 (DPP-3) inhibitor with an IC50 value of 24 µg/mL. Fluostatin B is a fluorenone, which is found in Streptomyces.
    Fluostatin B
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Dipeptidyl Peptidase Isoform Comparison

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