2. PROTAC Metabolic Enzyme/Protease GPCR/G Protein
  3. PROTACs Dipeptidyl Peptidase GLP Receptor
  4. DeDPP4

DeDPP4 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.
(Pink: DPP-4 ligand (HY-A0023A); Blue: Cereblon ligand (HY-W763812); Black: linker (HY-W067489)).

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DeDPP4

DeDPP4 Chemical Structure

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DeDPP4 Related Antibodies

Top Publications Citing Use of Products

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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DPP-1 DPP-2 DPP-4 DPP-8 DPP-9

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Description

DeDPP4 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[1]. (Pink: DPP-4 ligand (HY-A0023A); Blue: Cereblon ligand (HY-W763812); Black: linker (HY-W067489)).

IC50 & Target[1]

Cereblon

 

DPP-4

 

In Vitro

DeDPP4 (10 μg/mL; 4 h) can be internalized into A549 cells via the endocytic pathway, and intracellular fluorescence is detectable after incubation at 10 μg/mL for 4 h[1].
DeDPP4 (0-1250 nM, 24-48 h) induces dose- and time-dependent degradation of DPP-4 in A549 cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

DeDPP4 Related Antibodies

Western Blot Analysis[1]

Cell Line: A549 human nonsmall cell lung cancer cells
Concentration: 0, 5, 25, 125, 625, 1250 nM (24 h incubation); 0, 1, 2, 3, 5, 10 μM (24 h incubation); 500 nM (4-48 h incubation); 2 μM (1-48 h incubation)
Incubation Time: 24 h (5-1250 nM, 1-10 μM); 4-48 h (500 nM); 1-48 h (2 μM)
Result: Induced dose-dependent DPP-4 degradation in A549 cells, with pronounced efficacy at concentrations above 625 nM;
Showed a slight hook effect at 1-10 μM.
Induced time-dependent degradation, with increasing efficiency over 48 h at both 500 nM and 2 μM, consistent with PROTAC-mediated degradation kinetics.

Immunofluorescence[1]

Cell Line: A549 human nonsmall cell lung cancer cells
Concentration: 500 nM
Incubation Time: 24 h
Result: Caused a marked decrease in red DPP-4 fluorescence intensity in treated cells compared to the control group.
In Vivo

DeDPP4 (5-10 mg/kg; i.v.; single dose, every 2 days; 4 weeks) exerts dose-dependent, sustained glucose-lowering effects in db/db mice with type 2 diabetes, with 10 mg/kg i.v. maintaining reduced blood glucose for over 60 h, improving insulin sensitivity, preserving pancreatic β-cell function, regulating lipid metabolism, and protecting against organ injury via DPP-4 protein degradation[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: leptin receptor-deficient (db/db) (10-week-old, male)[1]
Dosage: 5 mg/kg (4-week study); 10 mg/kg (single-dose efficacy study; 4-week study)
Administration: i.v.; every 2 days; 4 weeks (5 mg/kg, 10 mg/kg 4-week study); i.v.; single dose (10 mg/kg efficacy longevity study)
Result: Maintained reduced blood glucose levels for over 60 h, with sustained hypoglycemia observed for up to 48 h (10 mg/kg single dose).
Reduced fasting blood glucose levels more effectively than 5 mg/kg DeDPP4, and lowered hemoglobin A1c (HbA1c) levels to ~7% after 4 weeks of treatment (10 mg/kg).
Reduced blood glucose to 10.6 mmol/L within 60 min during OGTT, with a significantly lower area under the blood glucose curve (AUC) than the model group (10 mg/kg).
Reduced the homeostasis model assessment of insulin resistance (HOMA-IR) more effectively than alogliptin, and preserved pancreatic β-cell function (HOMA-β) (10 mg/kg).
Significantly increased serum glucagon-like peptide-1 (GLP-1) levels compared to alogliptin (10 mg/kg).
Reduced serum levels of total cholesterol (TC), triglycerides (TG), low-density lipoprotein cholesterol (LDL-C), and free fatty acids (FFA) more effectively than 5 mg/kg DeDPP4 or alogliptin, while increasing high-density lipoprotein cholesterol (HDL-C) (10 mg/kg).
Significantly reduced serum alanine aminotransferase (ALT), aspartate aminotransferase (AST), blood urea nitrogen (BUN), and creatinine (CREA) levels (10 mg/kg).
Preserved pancreatic islet morphology with increased β-cell mass and reduced α/β cell ratio (10 mg/kg).
Induced a greater reduction in hepatic DPP-4 protein levels than 5 mg/kg DeDPP4 (10 mg/kg).
Molecular Weight

710.74

Formula

C36H38N8O8
SMILES

O=C(N[C@H]1CN(C(N2CC3=CC=CC=C3C#N)=CC(N(C2=O)C)=O)CCC1)CCOCCNC4=CC=CC(C5=O)=C4C(N5[C@@H](CC6)C(NC6=O)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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DeDPP4 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

DeDPP4DeDPP 4DeDPP-4PROTACsDipeptidyl PeptidaseGLP ReceptorDPPDPP-4 PROTAC degraderA549 cellsleptin receptor-deficient (db/db) micetype 2 diabetesnon-small cell lung cancerInhibitorinhibitorinhibit

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