PROTAC STING degrader-3
Based on 1 Customer Validation
PROTAC STING degrader-3 is a STING PROTAC degrader (DC50: 0.62 μM). PROTAC STING degrader-3 induces STING degradation via the ubiquitin-proteasome pathway. PROTAC STING degrader-3 exerts anti-inflammatory effects by inhibiting STING/TBK1/NF-κB signaling. PROTAC STING degrader-3 has renal protective effects and can be used in the study of acute kidney injury (AKI).
(Pink: STING ligand (HY-47709); Blue: Cereblon ligand (HY-41547); 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。
- 純度 : 98.35%
- CAS 番号: 3109967-69-0
- 分子式: C37H36N8O10
- 分子量:752.73
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
製品説明
体外実験
PROTAC STING degrader-3 (ST9) (0.08-10 μM; 2-48 h) potently degrades STING protein in THP-1 cells with a DC50 of 0.62 μM, acting via a ubiquitin-proteasome-dependent mechanism, and shows time-dependent degradation activity[1].
ST9 (1.25-5 μM; 24 h) blocks the STING/NF-κB downstream signaling axis in Cisplatin (HY-173940)-stimulated HK-2 cells by degrading STING, thereby reducing inflammatory factor expression[1].
ST9 (1.25-20 μM; 24 h) demonstrates selective degradation of STING protein in THP-1 cells, with no significant effect on AKT, STAT3, AMPK, ERK, or LKB1 levels[1].
ST9 (0.5-120 μM; 24 h) has a favorable in vitro safety profile, with no significant cytotoxicity in most normal cell lines and only mild effects at high concentrations in BV2 cells[1].
ST9 (1.25-5 μM; 24 h) inhibits ROS formation and P65 nuclear translocation in Cisplatin-stimulated HK-2 cells, contributing to its anti-inflammatory effects[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:THP-1
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Concentration:0.08 μM, 0.15 μM, 0.3 μM, 0.6 μM, 1.25 μM, 2.5 μM, 5 μM, 10 μM
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Incubation Time:2 h,4 h, 8 h, 12 h, 24 h, 48 h;
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Result:Degraded 90.6% of STING protein at 5 μM for 24 h.
Exhibited a DC50 of 0.62 μM for STING degradation in THP-1 cells.
Induced time-dependent STING degradation, with degradation starting at 2 h and reaching maximum at 48 h.
Was blocked by the proteasome inhibitor MG132 but not by the lysosome inhibitor bafilomycin A1 in mediating STING degradation.
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Cell Line:HK-2 (cisplatin-stimulated)
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Concentration:1.25-5 μM (co-incubated with 5 μM cisplatin)
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Incubation Time:24 h
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Result:Reduced cisplatin-induced ROS levels in a concentration-dependent manner.
Decreased cisplatin-induced P65 nuclear translocation in a concentration-dependent manner.
Parmacokinetics
| Species | Dose | Route | AUC0-t | AUC0-∞ | MRT0-t | MRT0-∞ | T1/2 | Tmax | CL | Vz | Cmax |
|---|---|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 2 mg/kg | i.v. | 728.9 μg·h/mL | 729.5 μg·h/mL | 0.20 h | 0.21 h | 0.86 h | 0.08 h | 3.2 L/h/kg | 3.9 L/kg | 2393.9 μg/mL |
体内実験
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 [1]
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Dosage:25 mg/kg, 50 mg/kg
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Administration:i.p.; daily; for 4 days
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Result:Suppressed the expression of STING proteins as well as P-TBK1 and P-P65.
Inflammatory factors (IFN-β, CXCL10, IL-6) in the serum of mice were significantly reduced.
化学情報
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CAS 番号 3109967-69-0
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性状 Solid
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分子量 752.73
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分子式 C37H36N8O10
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Color Light yellow to yellow
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SMILES
O=C(C1=CC=C([N+]([O-])=O)O1)NC2=CC=C(NC(/C=C/C(N3CCN(CC4CN(C5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)CC4)CC3)=O)=O)C=C2
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
体外:
DMSO : 100 mg/mL (132.85 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.32 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
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- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.3285 mL | 6.6425 mL | 13.2850 mL | 33.2124 mL |
| 5 mM | 0.2657 mL | 1.3285 mL | 2.6570 mL | 6.6425 mL | |
| 10 mM | 0.1328 mL | 0.6642 mL | 1.3285 mL | 3.3212 mL | |
| 15 mM | 0.0886 mL | 0.4428 mL | 0.8857 mL | 2.2142 mL | |
| 20 mM | 0.0664 mL | 0.3321 mL | 0.6642 mL | 1.6606 mL | |
| 25 mM | 0.0531 mL | 0.2657 mL | 0.5314 mL | 1.3285 mL | |
| 30 mM | 0.0443 mL | 0.2214 mL | 0.4428 mL | 1.1071 mL | |
| 40 mM | 0.0332 mL | 0.1661 mL | 0.3321 mL | 0.8303 mL | |
| 50 mM | 0.0266 mL | 0.1328 mL | 0.2657 mL | 0.6642 mL | |
| 60 mM | 0.0221 mL | 0.1107 mL | 0.2214 mL | 0.5535 mL | |
| 80 mM | 0.0166 mL | 0.0830 mL | 0.1661 mL | 0.4152 mL | |
| 100 mM | 0.0133 mL | 0.0664 mL | 0.1328 mL | 0.3321 mL |
PROTAC STING degrader-3 関連分類
HY-173414 関連分類
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