ADAR1i-124
Based on 1 Customer Validation
ADAR1i-124 is an A-to-I RNA editing inhibitor by inhibiting the catalytic activities of both ADAR1p150 and ADAR1p110. ADAR1i-124 activates type I interferon (IFN) and ZBP1 pathways and dose-dependently inhibits viability across different types of cancer cell lines. ADAR1i-124 can induce cells apoptosis and necroptosis. ADAR1i-124 can be used for the research of cancer, such as cutaneous melanoma and ovarian cancer.
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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: 98.71%
- 分子式: C17H12ClN3O2
- 分子量:325.75
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保管条件:
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
DNA/RNA Synthesis アイソフォーム固有の製品をすべて表示
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生物活性
ADAR1i-124 (0-200 μM; 2 h) potently inhibits ADAR1p150-mediated A-to-I RNA editing in vitro with IC50 values of 8.8 μM (position 2) and 6.5 μM (position 5)[1].
ADAR1i-124 (300 μM; 2 h) does not inhibit ADAR2-mediated A-to-I RNA editing in vitro[1].
ADAR1i-124 binds selectively to ADAR1p110 with higher affinity than ADAR2 and does not bind to GAPDH[1].
ADAR1i-124 (10 μM; 12 h) induces unedited dsRNA located with MDA5 within the filament structures in mouse Yumm1.7 cutaneous melanoma cells[1].
ADAR1i-124 (10 μM; 12 h) decreases A-to-I editing and prompts the transition of certain dsRNAs from A-form to Z-form in Yumm1.7 cells[1].
ADAR1i-124 (48 h) induces dose-dependent cytotoxicity against mouse (Yumm1.7 CM, HSG2 OC) and human (WM4223 AM, WM3000 CM) cancer cells with IC50 values of 2.3, 1.2, 1.1 and 6.6 μM[1].
ADAR1i-124 (10 μM; 24 h) activates IFN signaling in Yumm1.7 melanoma and HGS2 OC cells[1].
ADAR1i-124 (10 μM; 24 h) induces apoptosis in HeLa and Yumm1.7 cells and also induces necroptosis activated by the ZBP1 pathway in Yumm1.7 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Yumm1.7 melanoma and HGS2 OC cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Upre-gulated expression of IFN-stimulated genes such as Ifih1 (MDA5), Cxcl9, and Cxcl10.
化学情報
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性状 Solid
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分子量 325.75
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分子式 C17H12ClN3O2
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Color White to off-white
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SMILES
OCN1C(C(NC2=CC=C(C#N)C=C2)=O)=C(Cl)C3=C1C=CC=C3
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶剤 & 溶解度
DMSO : 100 mg/mL (306.98 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 (protect from light). 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 (protect from light). 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)
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 (7.67 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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 (252 KB)
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- Portuguese - PT (252 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 (protect from light). 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.0698 mL | 15.3492 mL | 30.6984 mL | 76.7460 mL |
| 5 mM | 0.6140 mL | 3.0698 mL | 6.1397 mL | 15.3492 mL | |
| 10 mM | 0.3070 mL | 1.5349 mL | 3.0698 mL | 7.6746 mL | |
| 15 mM | 0.2047 mL | 1.0233 mL | 2.0466 mL | 5.1164 mL | |
| 20 mM | 0.1535 mL | 0.7675 mL | 1.5349 mL | 3.8373 mL | |
| 25 mM | 0.1228 mL | 0.6140 mL | 1.2279 mL | 3.0698 mL | |
| 30 mM | 0.1023 mL | 0.5116 mL | 1.0233 mL | 2.5582 mL | |
| 40 mM | 0.0767 mL | 0.3837 mL | 0.7675 mL | 1.9186 mL | |
| 50 mM | 0.0614 mL | 0.3070 mL | 0.6140 mL | 1.5349 mL | |
| 60 mM | 0.0512 mL | 0.2558 mL | 0.5116 mL | 1.2791 mL | |
| 80 mM | 0.0384 mL | 0.1919 mL | 0.3837 mL | 0.9593 mL | |
| 100 mM | 0.0307 mL | 0.1535 mL | 0.3070 mL | 0.7675 mL |