Thienopyridone
Based on 1 publication(s) in Google Scholar
Thienopyridone is a potent and selective phosphatase of regenerating liver (PRL) phosphatase inhibitor with IC50s of 173 nM, 277 nM and 128 nM for PRL-1, PRL-2, and PRL-3, respectively. Thienopyridone shows minimal effects on other phosphatases. Thienopyridone induces p130Cas cleavage and apoptosis and has anticancer effects.
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- 純度: 95.14%
- CAS 番号: 1018454-97-1
- 分子式: C13H10N2OS
- 分子量:242.30
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
MedChemExpress(MCE)の使用を引用している文献 Thienopyridone
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生物活性
IC50: 173 nM (PRL-1), 277 nM (PRL-2) and 128 nM (PRL-3)[1]
Thienopyridone shows significant inhibition of tumor cell anchorage-independent growth in soft agar. The EC50 values of the Thienopyridone are 3.29 μM and 3.05 μM for RKO and HT-29 cells, respectively[1].
Thienopyridone (1-75 μM; 24 hours; HeLa cells) treatment shows a dose-dependent down-regulation of total p130Cas in HeLa cells. Thienopyridone induces p130Cas and FAK cleavage leads to caspase-mediated cell apoptosis. Thienopyridone induces the cleavage of PARP and caspase-8[1].
Thienopyridone (3.75-30 μM; 24 hours) significantly suppresses HUVEC migration but not proliferation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RKO and HT-29 cells
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Concentration:0.5 μM, 1.67 μM, 5 μM, 8.33 μM
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Incubation Time:14 days
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Result:Exhibited a dose-dependent inhibition in cancer cell anchorage-independent growth as measured by either colony number or colony size.
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Cell Line:HeLa cells
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Concentration:1 μM, 5 μM, 10 μM, 25 μM, 50 μM, 75 μM
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Incubation Time:24 hours
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Result:A dose-dependent down-regulation of total p130Cas was observed.
化学情報
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CAS 番号 1018454-97-1
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性状 Solid
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分子量 242.30
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分子式 C13H10N2OS
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Color Yellow to brown
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SMILES
O=C1C(C=C(C2=CC=CC=C2)S3)=C3C(N)=CN1
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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 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Sci Rep
Development of a high-throughput screening system targeting the protein-protein interactions between PRL and CNNM. [Abstract]2024 Oct 25;14(1):25432. PMID: 39455715
溶剤 & 溶解度
DMSO : 5 mg/mL (20.64 mM; ultrasonic and warming and adjust pH to 5 with HCl and heat to 80°C; 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (8.58 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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 (392 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.1271 mL | 20.6356 mL | 41.2712 mL | 103.1779 mL |
| 5 mM | 0.8254 mL | 4.1271 mL | 8.2542 mL | 20.6356 mL | |
| 10 mM | 0.4127 mL | 2.0636 mL | 4.1271 mL | 10.3178 mL | |
| 15 mM | 0.2751 mL | 1.3757 mL | 2.7514 mL | 6.8785 mL | |
| 20 mM | 0.2064 mL | 1.0318 mL | 2.0636 mL | 5.1589 mL |