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 (110)
Related Products (110)
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PB01
0 ImagesCat. No.: HY-170572CAS No.: 368434-78-0PB01 is a DPP-4 inhibitor with an IC50 of 15.66 nM. It effectively inhibits high glucose-induced ROS production and mitochondrial superoxide formation while significantly reducing cellular DPP-4 expression. PB01 can also significantly lower blood glucose levels in diabetic mice. Additionally, PB01 demonstrates good safety, exhibiting almost no cytotoxicity at a concentration of 100 μM. PB01 holds potential for research in the field of diabetes.
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ZY15557
0 ImagesCat. No.: HY-153522CAS No.: 1601480-12-9ZY15557 is a novel, competitive, long acting, orally active DPP-4 inhibitor, with a Ki of 5.53 nM. ZY15557 inhibits plasma DPP-4 activity. ZY15557 can be used in the research of type 2 diabetes.
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Vildagliptin-d7
0 ImagesCat. No.: HY-14291S1CAS No.: 1133208-42-0Synonyms: LAF237-d7; NVP-LAF 237-d7Vildagliptin-d7 is 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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ASP4000 hydrochloride
0 ImagesCat. No.: HY-111294CAS No.: 851389-35-0ASP4000 hydrochloride 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 hydrochloride reduces the degradation of active glucagon-like peptide-1 (GLP-1), thereby persistently increasing postprandial active GLP-1 levels and improving glycemic control. ASP4000 hydrochloride can be used in studies related to type 2 diabetes.
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DPP-4/GPR119 modulator 1
0 ImagesCat. No.: HY-146468CAS No.: 2411099-68-6DPP-4/GPR119 modulator 1 (Compound 22) is an orally active dipeptidyl peptidase IV (DPP-IV) inhibitor and GPR119 agonist. DPP-4/GPR119 modulator 1 shows blood glucose-lowering effect and moderate inhibition on hERG channel with an IC50 of 4.9 μM. DPP-4/GPR119 modulator 1 can be used for diabetes research. DPP-4/GPR119 modulator 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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HBK001
0 ImagesCat. No.: HY-182580CAS No.: 1942922-78-2HBK001 is an orally active and selective dual GPR119 agonist and DPP-IV inhibitor. HBK001 triggers cAMP production, PKA activation, CREB phosphorylation, glucose-stimulated insulin secretion, plasma incretin elevation, β-cell proliferation, and β-cell function gene up-regulation. HBK001 reduces blood glucose, ameliorates hyperglycemia, improves glucose tolerance, and enhances islet morphology. HBK001 can be used for the research of type 2 diabetes mellitus.
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Hypoglycemic agent 4
0 ImagesCat. No.: HY-180784Hypoglycemic agent 4 (Compound 5b) is a tetrahydroacridine derivative with orally active hypoglycemic activity. Hypoglycemic agent 4 has a good binding affinity for the key diabetic targets: DPP-IV, SGLT1, and GLUT2. Hypoglycemic agent 4 can inhibit glucose diffusion. Hypoglycemic agent 4 can reduce fasting blood sugar in Streptozotocin (HY-13753)-induced diabetic rats and its effect is comparable to Gliclazide (HY-B0753). Hypoglycemic agent 4 can be used for research of type 2 diabetes.
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Epibestatin hydrochloride
0 ImagesEpibestatin hydrochloride is an epimer of Bestatin (HY-B0134), a DPP4 inhibitor and protease inhibitor, with an IC50 of 17 μM against DPP4. As a stabilizer, Epibestatin hydrochloride binds to the cleft between 14-3-3 protein and plant proton pump PMA2, selectively stabilizing their interaction without affecting other 14-3-3 client proteins. Epibestatin hydrochloride triggers stomatal opening in leaf epidermis of Commelina communis. Epibestatin hydrochloride can be used in studies related to type 2 diabetes.
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DeDPP4
0 ImagesCat. No.: HY-182336DeDPP4 is a DPP-4 PROTAC degrader. DeDPP4 induces sustained elevation of glucagon-like peptide-1 (GLP-1), enhances glucose tolerance, causes persistent reduction of blood glucose, and achieves long-term blood glucose regulation in animal models of type 2 diabetes. DeDPP4 mediates dose-dependent DPP-4 depletion in cancer cells, and also targets and degrades DPP-4 in the liver and adipose tissues of animal models with type 2 diabetes. DeDPP4 can be used for the research of type 2 diabetes and non-small cell lung cancer.
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Linagliptin-13C,d3
0 ImagesCat. No.: HY-10284S1CAS No.: 1398044-43-3Synonyms: BI 1356-13C,d3Linagliptin-13C,d3 is the 13C- and deuterium labeled Linagliptin. Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM. Linagliptin-13C,d3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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DPP-4-IN-3
0 ImagesCat. No.: HY-146455CAS No.: 2402735-14-0DPP-4-IN-3 (Compound 5a) is a potent dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 0.75 nM. DPP-4-IN-3 shows excellent antioxidant and insulinotropic activity.
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DPP-8/9 probe-1
0 ImagesCat. No.: HY-D2327CAS No.: 3020859-80-4DPP-8/9 probe-1 (compound 20) is a fluorescent probe targeting Dipeptidyl Peptidase DPP8/9, which can be selectively labeled and visualized in vitro by fluorescence microscopy Active DPP8/9. DPP-8/9 probe-1 contains a nitrobenzoxadiazole (NBD) tag and has high affinity and selectivity for DPP8/9 over related S9 family members (IC50 of 210 nM and 15 nM, respectively).
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EOS34295
0 ImagesCat. No.: HY-189613EOS34295 is a dipeptidyl peptidase-IV (DPP-IV) inhibitor predicted to have oral activity. EOS34295 competitively binds to key residues in the active site of DPP-IV, inhibiting its enzymatic activity and blocking the degradation of incretins such as GLP-1/GIP, ultimately promoting insulin release to improve glycemic control. EOS34295 can be used in the study of type 2 diabetes.
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5-Hydroxy saxagliptin hydrochloride
0 ImagesCat. No.: HY-W741755A5-Hydroxy saxagliptin hydrochloride is an active metabolite of Saxagliptin (HY-10285) and a potent and selective DPP-4 inhibitor. 5-Hydroxy saxagliptin hydrochloride has Ki values of 2.6 nM and 2.9 nM for humans and cynomolgus monkeys, respectively. 5-Hydroxy saxagliptin hydrochloride can be used in the research of type 2 diabetes mellitus.
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Cyclocarin A
0 ImagesCat. No.: HY-N17777CAS No.: 1403937-45-0Cyclocarin A is a triterpenoid compound that can be isolated from the leaves of Cyclocarya paliurus. Cyclocarin A shows only weak inhibitory activity against α-glucosidase, lipase, DPP-IV, aldose reductase, and human cancer cell lines (IC50>10 μM).
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AMG-222
0 ImagesCat. No.: HY-111150CAS No.: 913978-37-7AMG-222 is a dipeptidyl peptidase IV (DPP-IV) inhibitor that exerts its inhibitory effect by tightly and reversibly binding to DPPIV. AMG 222 binds to human plasma proteins in a saturable and concentration-dependent manner, with a binding rate of 80.8% at 1 nM, while the binding rate decreases to 29.4% at concentrations above 100 nM. AMG-222 can be used in research related to diabetes.
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BMS-767778
0 ImagesCat. No.: HY-16656CAS No.: 915729-95-2BMS-767778 is an orally active and selective DPP4 inhibitor with Ki values of 0.94 nM, 4.9, 3.2 nM for DPP4, DPP8 and DPP9 respectively. BMS-767778 exhibits >3,000-fold selectivity over the related enzymes DPP8 and DPP9. BMS-767778 inhibits CYP-3A4 with IC50 of 5.2 μM. BMS-767778 significantly reduces blood glucose levels in high fat fed (HFD) ob/ob mice with safety profile. BMS-767778 can be used for diabetes mellitus research.
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DPP-4-IN-1
0 ImagesCat. No.: HY-151383CAS No.: 2215027-46-4DPP-4-IN-1 (compound d1) is a potent DPP-4 (dipeptidyl peptidase 4) inhibitor, with an IC50of 49 nM. DPP-4-IN-1 is a structurally analogs of Alogliptin (HY-A0023A). DPP-4-IN-1 can be used for diabetes research.
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DPP-4-IN-10
0 ImagesCat. No.: HY-162513CAS No.: 1123219-12-4DPP-4-IN-10 (compound 1) is a DPP-4 inhibitor. DPP-4-IN-10 is orally active. DPP-4-IN-10 blocks the degradation of GLP-1 and GIP, which may improve glycemic control in type 2 diabetes (T2MD).
