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

DeDPP4 是一种 DPP-4 PROTAC 降解剂。DeDPP4 可诱导胰高血糖素样肽-1 (GLP-1) 持续升高，增强葡萄糖耐量，使血糖持续降低，并在 2 型糖尿病动物模型中实现长期血糖调控。DeDPP4 可在癌细胞中介导剂量依赖性的 DPP-4 耗竭，还可在 2 型糖尿病动物模型的肝脏和脂肪组织中靶向降解 DPP-4。DeDPP4 可用于 2 型糖尿病、非小细胞肺癌的研究。
(粉色: DPP-4 配体 (HY-A0023A)；蓝色: Ligands for E3 Ligase 和 Cereblon 配体 (HY-W763812)；黑色: 连接子 (HY-W067489))。

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DeDPP4

DeDPP4 Chemical Structure

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DeDPP4 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

查看所有亚型
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

查看 Dipeptidyl Peptidase 亚型特异性产品:

查看所有亚型
DPP-1 DPP-2 DPP-4 DPP-8 DPP-9

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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: Ligands for E3 Ligase and Cereblon ligand (HY-W763812); Black: linker (HY-W067489)).

IC50 & Target[1]

Cereblon

 

DPP-4

 

体外研究
(In Vitro)

DeDPP4 (10 μg/mL; 4 h) 可通过内吞途径被内化进入 A549 细胞，在 10 μg/mL 浓度下孵育 4 h 后可检测到细胞内荧光[1]。
DeDPP4 (0-1250 nM, 24-48 h) 可在 A549 细胞中诱导 DPP-4 呈剂量和时间依赖性降解[1]。

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

DeDPP4 相关抗体:

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.
体内研究
(In Vivo)

DeDPP4 (5-10 mg/kg；静脉注射；单次给药，每 2 天 1 次；持续 4 周) 在 2 型糖尿病 db/db 小鼠中发挥剂量依赖性的持久降糖作用，其中 10 mg/kg 静脉注射可使血糖维持降低状态超过 60 h，同时可改善胰岛素敏感性、保护胰腺 β 细胞功能、调节脂质代谢，并通过降解 DPP-4 蛋白发挥器官损伤保护作用[1]。

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).
分子量

710.74

Formula

C36H38N8O8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

DeDPP4 相关分类

  • 摩尔计算器

  • 稀释计算器

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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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