JYQ-194
Based on 1 Customer Validation
JYQ-194 is a PROTAC degrader that selectively induces PARK7 degradation by recruiting cereblon. JYQ-194 induces proteasome-dependent degradation of PARK7 in human tumor cells. JYQ-194 is applicable to research related to Parkinson's disease and cancer.
(Pink: ligand (HY-163563); Blue: Cereblon ligand (HY-10984); Black: linker (HY-W017440)).
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 : 98.05%
- CAS 番号: 3117543-71-9
- 分子式: C39H38FN11O8S
- 分子量:839.85
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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
- 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
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生物活性
製品説明
IC50 & Target
[1]|
PARK7 |
体外実験
JYQ-194 (0.1-5 μM; 8 h) dose-dependently induces PARK7 degradation in HeLa, H1299, and MCF7 human tumor cell lines[1].
JYQ-194 (5 μM; 1-24 h) induces PARK7 degradation in A549 cells starting at 4 h, with maximum degradation achieved by 8 h and sustained for up to 24 h[1].
JYQ-194 (5 μM; 8 h post-4 h pretreatment) induces PARK7 degradation in A549 cells that depends on ternary complex formation with CRBN and PARK7, as well as functional proteasomal activity[1].
JYQ-194 (5 μM; 8 h) selectively induces degradation of PARK7 in A549 cells, with secondary effects on a small number of additional proteins, including TM7SF3, DOP1B, and HINT2[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 human lung adenocarcinoma cells
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Concentration:0.1, 0.5, 1, 2, 5 μM
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Incubation Time:8 h
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Result:Induced dose-dependent degradation of PARK7, starting at 0.1 μM.
Achieved a maximum degradation of ~80% relative to DMSO control at 5 μM.
Caused statistically significant reductions at all tested concentrations.
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Cell Line:HeLa, H1299, MCF7 human tumor cell lines
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Concentration:0.1, 0.5, 1, 2, 5 μM
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Incubation Time:8 h
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Result:Induced dose-dependent degradation of PARK7 in all three tested tumor cell lines.
Caused visible reduction of PARK7 protein levels at increasing compound concentrations.
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Cell Line:A549 human lung adenocarcinoma cells
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Concentration:5 μM
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Incubation Time:1, 4, 8, 12, 24 h
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Result:Triggered PARK7 degradation first observed at 4 h after treatment.
Reached maximum degradation levels by 8 h.
Maintained consistent degradation levels through 24 h.
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Cell Line:A549 human lung adenocarcinoma cells
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Concentration:5 μM (Pomalidomide (HY-10984) pretreatment); 10 μM (MG-132 (HY-13259) pretreatment); 5 μM (JYQ-194 treatment)
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Incubation Time:4 h (pretreatment); 8 h (JYQ-194 post-pretreatment)
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Result:Had induced PARK7 degradation completely abolished by pretreatment with pomalidomide or MG-132.
Demonstrated reliance on CRBN binding, PARK7 binding, and proteasomal activity for PARK7 degradation.
化学情報
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CAS 番号 3117543-71-9
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性状 Solid
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分子量 839.85
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分子式 C39H38FN11O8S
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Color Light yellow to yellow
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SMILES
O=C([C@H]1CN(C#N)CC1)NC(S2)=NC3=C2CN(C(C4=C(F)C=CC(N5C=C(COCCOCCNC6=C(C(N(C7CCC(NC7=O)=O)C8=O)=O)C8=CC=C6)N=N5)=C4)=O)CC3
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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 : 25 mg/mL (29.77 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 (2.98 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 (280 KB)
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SDS (254 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.1907 mL | 5.9534 mL | 11.9069 mL | 29.7672 mL |
| 5 mM | 0.2381 mL | 1.1907 mL | 2.3814 mL | 5.9534 mL | |
| 10 mM | 0.1191 mL | 0.5953 mL | 1.1907 mL | 2.9767 mL | |
| 15 mM | 0.0794 mL | 0.3969 mL | 0.7938 mL | 1.9845 mL | |
| 20 mM | 0.0595 mL | 0.2977 mL | 0.5953 mL | 1.4884 mL | |
| 25 mM | 0.0476 mL | 0.2381 mL | 0.4763 mL | 1.1907 mL |
JYQ-194 関連分類
HY-163564 関連分類
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