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.
Dipeptidyl Peptidase Isoform Specific Products
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Dipeptidyl Peptidase Inhibitors
(213)
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Dipeptidyl Peptidase Antagonist
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Dipeptidyl Peptidase Activator
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Dipeptidyl Peptidase Controls
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Dipeptidyl Peptidase Substrates
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DPP IV/CD26 Proteins
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Dipeptidyl Peptidase Related Products (240)
Related Products (240)
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Recombinant Proteins (9)
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Antibodies (1)
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Dipeptidyl Peptidase Isoform Comparison
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Sitagliptin hydrochloride
0 ImagesCat. No.: HY-13749ECAS No.: 486459-71-6Synonyms: MK-0431 hydrochlorideSitagliptin (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.
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SGP8
0 ImagesCat. No.: HY-P6177CAS No.: 855790-98-6SGP8 (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).
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DPP-4-IN-12
0 ImagesCat. No.: HY-169110DPP-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.
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Pro-Arg-AMC
0 ImagesCat. No.: HY-P4345CAS No.: 546103-85-9Pro-Arg-AMC is a peptide substrate of DPAP1.
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DPP-4-IN-8
0 ImagesCat. No.: HY-155027DPP-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).
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Sitagliptin (Standard)
0 ImagesCat. No.: HY-13749RCAS No.: 486460-32-6Synonyms: MK-0431 (Standard)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.
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MK-789
0 ImagesCat. No.: HY-111282CAS No.: 85394-14-5MK-789 is a competitive reversible inhibitor of dehydropeptidase I (DHP-I). MK-789 competitively blocks the entry of N-formimidoylthienamycin into proximal tubular cells, thereby inhibiting its renal metabolism. MK-789 shifts the renal excretion pathway of N-formimidoylthienamycin to glomerular filtration only, increasing its urinary recovery rate and renal clearance. MK-789 is applicable to studies on renal metabolism and pharmacokinetics.
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Trelagliptin succinate (Standard)
0 ImagesSynonyms: SYR-472 succinate (Standard)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).
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(S)-Sitagliptin phosphate (Standard)
0 ImagesCat. No.: HY-13749CRCAS No.: 823817-58-9Synonyms: (S)-MK-0431 phosphate (Standard)(S)-Sitagliptin phosphate (Standard) ((S)-MK-0431 phosphate (Standard)) is the analytical standard of (S)-Sitagliptin (phosphate) (HY-13749C). This product is intended for research and analytical applications. (S)-Sitagliptin phosphate ((S)-MK-0431 phosphate) is the S-isomer of Sitagliptin phosphate (HY-13749A). Sitagliptin phosphate (MK-0431 phosphate) is a potent DPP4 inhibitor. (S)-Sitagliptin phosphate can be used in diabetes research.
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MPO-IN-6
0 ImagesCat. No.: HY-163332MPO-IN-6 (compound ADC) is an electrophile with good antioxidant and anti-inflammatory properties. MPO-IN-6 is a myeloperoxidase (MPO), dipeptidyl peptidase-4 (DPP-4), and α-glucosidase (α-GD) inhibitor with IC50s of 10 μM, 31.02 μM, and 46.05 μM, respectively. MPO-IN-6 is a potential cardiovascular preventive agent.
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SGLT2-IN-5
0 ImagesCat. No.: HY-180527SGLT2-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.
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Teneligliptin (Standard)
0 ImagesSynonyms: MP-513 (Standard)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.
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2-Methoxy-5-acetoxy-fruranogermacr-1(10)-en-6-one
0 Images2-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.
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DPP-4-IN-15
0 ImagesCat. No.: HY-170800CAS No.: 3035300-36-5DPP-4-IN-15 (Compound 22) is a non-competitive inhibitor of dipeptidyl peptidase-4 (DPP-4) with an IC50 of 8.24 μM.
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Saxagliptin hydrate (Standard)
0 ImagesCat. No.: HY-10285ARCAS No.: 945667-22-1Synonyms: BMS-477118 hydrate (Standard)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.
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DPP-4-IN-17
0 ImagesCat. No.: HY-175590DPP-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).
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Vildagliptin (Standard)
0 ImagesSynonyms: LAF237 (Standard); NVP-LAF 237 (Standard)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.
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Sitagliptin-d6
0 ImagesCat. No.: HY-13749S3CAS No.: 1133211-99-0Synonyms: MK-0431-d6Sitagliptin-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.
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(rel)-Saxagliptin-13C,d2 TFA
0 ImagesCat. No.: HY-10285S1CAS No.: 2012595-09-2Synonyms: (rel)-BMS-477118-13C,d2 TFA(rel)-Saxagliptin-13C,d2 ((rel)-BMS-477118-13C,d2) TFA is 13C-labeled Saxagliptin (HY-10285).
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DPP-IV-IN-2 (Standard)
0 ImagesCat. No.: HY-108319RCAS No.: 136259-18-2DPP-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.
