DPP-4
Dipeptidyl peptidase-4 (DPP-4), also known as CD26, is a membrane-associated and soluble serine exopeptidase that cleaves peptides containing alanine or proline at the penultimate N-terminal position, thereby regulating the biological activity of multiple peptide hormones and signaling molecules[1][2]. Mechanistically, DPP-4 is a key regulator of the incretin pathway because it rapidly degrades the active forms of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), generating truncated products with markedly reduced biological activity and limiting incretin-mediated glucose control[3][4][5]. Through this enzymatic process, DPP-4 influences insulin secretion, glucagon regulation, and systemic glucose homeostasis, making it a central component of metabolic signaling networks relevant to type 2 diabetes mellitus (T2DM) and related metabolic disorders[4][6][7]. In disease contexts, elevated DPP-4 activity has been associated with insulin resistance, inflammation, obesity, and T2DM, supporting its use as a mechanistic target and biomarker in metabolic research models[2]. Compared with related members of the dipeptidyl peptidase family, DPP-4 is distinguished by its well-characterized role in incretin degradation and its dual function as both an enzymatic regulator and a cell-surface signaling molecule, which contributes to its broad physiological relevance[1][2]. For experimental applications, selective DPP-4 inhibitors are widely used to prolong endogenous GLP-1 and GIP activity, enhance glucose-dependent insulin secretion, and improve glycemic control, providing robust pharmacological tools for investigating incretin biology and metabolic disease mechanisms[6][7][8].
References:
- [1]. Huang P K, Lin S R, Chang C H, et al. Natural phenolic compounds potentiate hypoglycemia via inhibition of Dipeptidyl peptidase IV[J]. Scientific Reports, 2019, 9(1): 15585.
- [2]. Pechmann LM, et al. The multiple actions of dipeptidyl peptidase 4 (DPP-4) and its pharmacological inhibition on bone metabolism: a review. Diabetol Metab Syndr. 2024 Jul 25;16(1):175. [Content Brief]
- [3]. Kieffer TJ, et al. Degradation of glucose-dependent insulinotropic polypeptide and truncated glucagon-like peptide 1 in vitro and in vivo by dipeptidyl peptidase IV. Endocrinology. 1995 Aug;136(8):3585-96. [Content Brief]
- [4]. Müller TD, et al. Glucagon-like peptide 1 (GLP-1). Mol Metab. 2019 Dec;30:72-130. [Content Brief]
- [5]. Zheng Z, et al. Glucagon-like peptide-1 receptor: mechanisms and advances in therapy. Signal Transduct Target Ther. 2024 Sep 18;9(1):234. [Content Brief]
- [6]. Ahren B. DPP-4 inhibitors[J]. Best Practice & Research Clinical Endocrinology & Metabolism, 2007, 21(4): 517-533.
- [7]. Deacon C F. Peptide degradation and the role of DPP-4 inhibitors in the treatment of type 2 diabetes[J]. Peptides, 2018, 100: 150-157.
- [8]. Dalle S, Burcelin R, Gourdy P. Specific actions of GLP-1 receptor agonists and DPP4 inhibitors for the treatment of pancreatic 尾-cell impairments in type 2 diabetes[J]. Cellular signalling, 2013, 25(2): 570-579.
All Product Categories
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DPP-4 Related Products (109)
Related Products (109)
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H-Gly-Pro-Hyp-OH acetate
0 ImagesCat. No.: HY-A0299ACAS No.: 103192-50-3H-Gly-Pro-Hyp-OH acetate is a dipeptidyl peptidase 4 (DPP-4) inhibitor with an IC50 value of 2.51 mM. H-Gly-Pro-Hyp-OH acetate is promising for research of diabetes.
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ASP4000 free base
0 ImagesCat. No.: HY-167075CAS No.: 851510-67-3ASP4000 free base is an orally effective dipeptidyl peptidase 4 (DPP4) inhibitor, with an IC50 value of 2.25 nM against human recombinant DPP4, and exhibits hypoglycemic activity. By inhibiting DPP4 activity, ASP4000 free base reduces the degradation of active glucagon-like peptide-1 (GLP-1), thereby persistently increasing postprandial active GLP-1 levels and improving glycemic control. ASP4000 free base can be used in studies related to type 2 diabetes.
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Anthraquinone-2-carboxylic acid (Standard)
0 ImagesCat. No.: HY-W031757RCAS No.: 117-78-2Anthraquinone-2-carboxylic acid (Standard) is the analytical standard of Anthraquinone-2-carboxylic acid (HY-W031757). This product is intended for research and analytical applications. Anthraquinone-2-carboxylic acid is an orally active anthraquinone compound and Antibacterial agent. Anthraquinone-2-carboxylic acid can be isolated from Bajitian. Anthraquinone-2-carboxylic acid inhibits the activation of DPP-IV, COX-2, NF-κB and AP-1. Anthraquinone-2-carboxylic acid blocks IAV-induced activation of the RIG-I/STAT1 pathway, alleviates IAV-mediated weight loss, and protects against lethal IAV infection. Anthraquinone-2-carboxylic acid inhibits the growth of various Staphylococcus strains. It possesses potent anti-inflammatory, immunomodulatory, analgesic and antibacterial activities.\n
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Lupinalbin A
0 ImagesCat. No.: HY-N4069CAS No.: 98094-87-2Synonyms: Boeravinone LLupinalbin A (Boeravinone L) is a dipeptidyl peptidase 4 (DPP4) and α-glucosidase inhibitor with IC50 values of 45.2 and 53.4 µM, respectively. Lupinalbin A exhibits antidiabetic activity.
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Vildagliptin-d3
0 ImagesCat. No.: HY-14291SCAS No.: 1217546-82-1Synonyms: LAF237-d3; NVP-LAF 237-d3Vildagliptin-d3 is the deuterium labeled Vildagliptin. 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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HTS13517
0 ImagesCat. No.: HY-119266CAS No.: 91533-02-7HTS13517 is a DPP4 inhibitor, with an IC50 of 10.73 μM.
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DPP-4-IN-16
0 ImagesCat. No.: HY-174832DPP-4-IN-16 (Compound 92) is a potent dipeptidyl peptidase-4 (DPP-4) inhibitor (IC50=0.8 nM). DPP-4-IN-16 inhibits DPP-4-mediated degradation of incretins (e.g., GLP-1 and GIP) to promote insulin secretion and reduce blood glucose. DPP-4-IN-16 is promising for research of type 2 diabetes.
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TS-021
0 ImagesCat. No.: HY-U00346ACAS No.: 667865-69-2TS-021 is a selective，orally active，reversible and long-acting DPP-IV inhibitor，and exhibits significant inhibition selectivity against DPP-8 (> 600 fold)，DPP-9 (> 1200 fold) and other peptidases (> 15,000 fold). TS-021 inhibits DPP-IV activity in human plasma with an IC50 value of 5.34 nM. TS-021 has long-term persistent plasma drug concentration and potent antihyperglycemic activity，and increases in the active form of GLP-1.
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Sennidin B (Standard)
0 ImagesSennidin B Standard is the analytical standard of Sennidin B (HY-N6935). This product is intended for research and analytical applications. Sennidin B is an anthraquinone compound isolated from Cassia angustifolia. Sennidin B is a DPP-4 inhibitor with an IC50 of 39.39 μM. Sennidin B is an insect chitinase inhibitor with a Ki of 80 nM against OfChi-h. Sennidin B competitively inhibits chitinase activity by forming π-π stacking interactions with key tryptophan residues in the active site through a folded conformation. Sennidin B activates PI3K/Akt to promote glucose uptake in adipocytes. Sennidin B can be used for the development of biopesticides and research on type 2 diabetes and metabolism-related signaling pathways.
