WY165
Based on 1 Customer Validation
WY165 is a bifunctional molecule comprising TR79, an activator of the mitochondrial protease complex caseinolytic protease P (ClpP), linked to desthiobiotin. WY165 mediates selective degradation of monomeric streptavidin (mSA) and its fusion proteins localized to the mitochondrial matrix with a DC50 of 197 nM. WY165 restores mitochondrial morphology by reducing the level of mSA fused to short transmembrane protein 1 (mSA-STMP1) in cells overexpressing mSA-STMP1. WY165 can be used for research in cancer, neurodegenerative diseases, cardiovascular diseases, and metabolic diseases.
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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: 99.00%
- 分子式: C46H61F3N8O9
- 分子量:927.02
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保管条件:
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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
生物活性
caseinolytic protease P (ClpP), monomeric streptavidin (mSA)
WY165 (10-10000 nM; 24 h) decreases mSA in a dose-dependent manner[1].
WY165's (1 μM; 24 h) mSA degradation activity is inhibited by excess desthiobiotin (1 mM), suggesting that the formation of the [mSA-WY165-ClpP] ternary complex is required[1].
WY165 (0.3-30 μM; 2-12 h) reduced mitochondrial mSA levels in HeLa and MCF7 cells transiently expressing mitochondrial cox8-mSA-FLAG in a dose- and time-dependent manner, with DC50 values for mSA of 4.8 μM and 0.96 μM, respectively[1].
WY165-induced (10 μM; 48 h) degradation of mSA depends on ClpP in HeLa cells[1].
WY165 (1-30 μM) decreases mSA-STMP1 in a dose-dependent manner in HeLa cells transiently expressing cox8-His6-mSA-STMP1-FLAG[1].
WY165 (1 μM) successfully restores the changes in mitochondrial morphology in HeLa cells expressing mSA-STMP1 and do not change mitochondrial morphology in HeLa cells not expressing mSA-STMP1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HeLa cells transiently expressing mitochondrial cox8-mSA-FLAG
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Concentration:1 μM; 3 μM; 10 μM; 30 μM
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Incubation Time:12 h
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Result:Successfully reduced the mSA level in the concentration of 10 μM and 30 μM.
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Cell Line:HeLa cells transiently expressing mitochondrial cox8-mSA-FLAG
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Concentration:10 μM
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Incubation Time:2 h; 4 h; 6 h; 12 h
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Result:Successfully reduced the mSA level upon 4 h treatment.
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Cell Line:MCF7 cells transiently expressing mitochondrial cox8-mSA-FLAG
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Concentration:0.3 μM; 1 μM; 3 μM; 10 μM; 30 μM
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Incubation Time:12 h
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Result:Significantly reduced the mSA level when concentration over 1 μM.
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Cell Line:MCF7 cells transiently expressing mitochondrial cox8-mSA-FLAG
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Concentration:3 μM
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Incubation Time:2 h; 4 h; 6 h; 12 h
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Result:Significantly reduced the mSA level upon 2 h treatment.
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Cell Line:HeLa cells with ClpP knockdown by transfection of siClpP
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Concentration:10 μM
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Incubation Time:48 h
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Result:Failed to degrade mSA in the presence of ClpP RNAi.
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Cell Line:HeLa cells transiently expressing cox8-His6-mSA-STMP1-FLAG
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Concentration:1 μM; 3 μM; 10 μM; 30 μM
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Incubation Time:48 h
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Result:Decreased mSA-STMP1 in a dose-dependent manner.
化学情報
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性状 Solid
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分子量 927.02
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分子式 C46H61F3N8O9
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Color Off-white to light yellow
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SMILES
O=C(COCCOCCOCCOCCNC(CCCCC[C@H]([C@@H](N1)C)NC1=O)=O)NCCCN2C(N(CC3=CC=C(C(F)(F)F)C=C3)C(C4=C2CCN(CC5=CC(C#N)=CC=C5)C4)=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
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
溶剤 & 溶解度
DMSO : 60 mg/mL (64.72 mM; ultrasonic and warming and heat to 60°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, 6 months; -20°C, 1 month (sealed storage, away from moisture and 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 (sealed storage, away from moisture and 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: ≥ 6 mg/mL (6.47 mM); Clear solution
This protocol yields a clear solution of ≥ 6 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (60.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 6 mg/mL (6.47 mM); Clear solution
This protocol yields a clear solution of ≥ 6 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (60.0 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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and 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 (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- 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 (sealed storage, away from moisture and 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 |
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| DMSO | 1 mM | 1.0787 mL | 5.3936 mL | 10.7873 mL | 26.9681 mL |
| 5 mM | 0.2157 mL | 1.0787 mL | 2.1575 mL | 5.3936 mL | |
| 10 mM | 0.1079 mL | 0.5394 mL | 1.0787 mL | 2.6968 mL | |
| 15 mM | 0.0719 mL | 0.3596 mL | 0.7192 mL | 1.7979 mL | |
| 20 mM | 0.0539 mL | 0.2697 mL | 0.5394 mL | 1.3484 mL | |
| 25 mM | 0.0431 mL | 0.2157 mL | 0.4315 mL | 1.0787 mL | |
| 30 mM | 0.0360 mL | 0.1798 mL | 0.3596 mL | 0.8989 mL | |
| 40 mM | 0.0270 mL | 0.1348 mL | 0.2697 mL | 0.6742 mL | |
| 50 mM | 0.0216 mL | 0.1079 mL | 0.2157 mL | 0.5394 mL | |
| 60 mM | 0.0180 mL | 0.0899 mL | 0.1798 mL | 0.4495 mL |
WY165 関連分類
HY-182964 関連分類
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