MH-06
MH-06 is an orally active 12-lipoxygenase (ALOX12) PROTAC degrader. MH-06 specifically binds to ALOX12 and recruits E3 ubiquitin ligase to mediate ubiquitination and degradation of the target protein. MH-06 inhibits the MAPK signaling pathway, reduces the production of reactive oxygen species (ROS), restores mitochondrial function, regulates macrophage polarization and decreases the release of pro-inflammatory cytokines. MH-06 can be used for the research of acute pancreatitis.
(Pink: 12-LOX ligand (HY-187183); Blue: Cereblon ligand (HY-10984); Black: linker).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C30H27N7O7
- 分子量:597.58
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
[1]|
12-LOX |
Cereblon |
体外実験
MH-06 (5.0-10.0 μM; 24 h) dose-dependently reduces the protein expression levels of pyroptosis markers Caspase-1, NLRP3 and ASC in LPS-induced inflammatory AR42J rat pancreatic exocrine cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LPS-induced inflammatory AR42J rat pancreatic exocrine cells
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Concentration:1.25, 2.5, 5.0, 10.0, 15.0, 20.0 μM
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Incubation Time:24 h
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Result:Nearly achieved complete degradation of ALOX12 protein at 10.0 μM.
Showed significant degradation activity at 5.0 μM, with almost complete degradation occurring at 10.0 μM and higher concentrations.
Confirmed dose-dependent reduction in ALOX12 protein levels relative to β-actin.
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Cell Line:LPS-induced inflammatory AR42J rat pancreatic exocrine cells
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Concentration:10.0 μM
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Incubation Time:24 h
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Result:Significantly inhibited the transcriptional levels of TNF-α, IL-6, and CCL2 compared to the LPS-induced control group.
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Cell Line:LPS-induced inflammatory AR42J rat pancreatic exocrine cells
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Concentration:5.0, 10.0 μM
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Incubation Time:24 h
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Result:Had no significant effect on total ERK and P38 protein levels.
Significantly inhibited the expression of phosphorylated ERK (p-ERK) and phosphorylated P38 (p-P38) in a concentration-dependent manner, with higher concentrations showing greater inhibitory activity.\nSignificantly reduced the protein expression levels of Caspase-1, NLRP3, and ASC in a concentration-dependent manner.
Showed the strongest inhibitory effect at 10.0 μM.
体内実験
Compared with single-dose administration, MH-06 (60 mg/kg; p.o.; administered twice) exerts superior preventive and therapeutic effects on caerulein-induced acute pancreatitis in C57BL/6J mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J mice (18-22 g, healthy)[1]
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Dosage:30 mg/kg; 60 mg/kg; 90 mg/kg
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Administration:p.o.; single dose
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Result:Reduced serum amylase, serum lipase, pancreatic trypsin activity, and pancreatic myeloperoxidase (MPO) activity in a dose-dependent manner.
Decreased serum amylase by 44.89%, serum lipase by 49.58%, pancreatic trypsin activity by 50.79%, and pancreatic MPO activity by 56.80% at 90 mg/kg compared to untreated cerulein-induced AP mice.
Alleviated pancreatic edema, inflammatory cell infiltration, and acinar cell necrosis in a dose-dependent manner, with the 90 mg/kg group showing the most significant improvement in pancreatic tissue damage.
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Animal Model:C57BL/6J mice (18-22 g, healthy)[1]
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Dosage:60 mg/kg
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Administration:p.o.; two doses: 1 hour pre-modeling and 6 hours post-final cerulein injection
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Result:Exerted a significantly stronger inhibitory effect on acute pancreatitis compared to the single intervention group, though its efficacy was slightly lower than that of the single 90 mg/kg MH-06 dose group.
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Animal Model:C57BL/6J mice (18-22 g, healthy)[1]
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Dosage:200 mg/kg; 300 mg/kg; 400 mg/kg
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Administration:p.o.; single dose
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Result:Showed no abnormal behavioral or physical manifestations in any dose group within 24 hours.
Maintained normal mental status, locomotor activity, food intake, and showed no significant body weight fluctuations over the 7-day observation period.
- Phagocytosis Functional Assay
- Mitochondrial membrane-potential fluorescent assay
- LPS-Induced Endotoxemia/Systemic Inflammation
- ROS/oxidative-stress fluorescent staining
- Mitochondrial membrane-potential and mitochondrial mass staining
- Primary monocyte-to-macrophage differentiation
- Research Protocol for Inflammation-related Diseases
化学情報
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分子量 597.58
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分子式 C30H27N7O7
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SMILES
O=C1CCC(C(N1)=O)N2C(C3=C(C(NC(CN4CCN(CC4)CC5=NC6=C(C(N5)=O)OC7=CC=CC=C76)=O)=CC=C3)C2=O)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
MH-06 関連分類
HY-187182 関連分類
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