GSK_WRN4
Based on 1 Customer Validation
GSK_WRN4 is an orally active WRN helicase inhibitor (pIC50=7.6). GSK_WRN4 induces DNA damage markers (p21, p-γH2AX, p-KAP1). GSK_WRN4 selectively inhibits microsatellite-unstable tumor growth in vitro and in vivo by inducing DNA double-strand breaks, particularly at expanded TA repeats and regions of DNA damage.
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- Pureté : 98.85%
- CAS No.: 2923008-66-4
- Formule: C16H20N2O4S
- Masse moléculaire:336.41
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Stockage: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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
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Helicase |
In Vitro
GSK_WRN4 (10 µM; 4 h) modifies only WRN Cys727 among 23,602 distinct cysteine-containing peptides in Jurkat cells[1].
GSK_WRN4 (72 h) preferentially inhibits the growth of MSI cancer cell lines (e.g., SW48) while sparing MSS models (e.g., SW620)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2923008-66-4
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Appearance Solid
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Masse moléculaire 336.41
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Formule C16H20N2O4S
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Color White to off-white
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SMILES
O=C1NC(C2CCCCC2)=CC=C1C(N[C@@H]3C=CS(=O)(C3)=O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (297.26 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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 (7.43 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.43 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 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.
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.
Pureté et documentation
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Fiche technique (273 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
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 | 2.9726 mL | 14.8628 mL | 29.7256 mL | 74.3141 mL |
| 5 mM | 0.5945 mL | 2.9726 mL | 5.9451 mL | 14.8628 mL | |
| 10 mM | 0.2973 mL | 1.4863 mL | 2.9726 mL | 7.4314 mL | |
| 15 mM | 0.1982 mL | 0.9909 mL | 1.9817 mL | 4.9543 mL | |
| 20 mM | 0.1486 mL | 0.7431 mL | 1.4863 mL | 3.7157 mL | |
| 25 mM | 0.1189 mL | 0.5945 mL | 1.1890 mL | 2.9726 mL | |
| 30 mM | 0.0991 mL | 0.4954 mL | 0.9909 mL | 2.4771 mL | |
| 40 mM | 0.0743 mL | 0.3716 mL | 0.7431 mL | 1.8579 mL | |
| 50 mM | 0.0595 mL | 0.2973 mL | 0.5945 mL | 1.4863 mL | |
| 60 mM | 0.0495 mL | 0.2477 mL | 0.4954 mL | 1.2386 mL | |
| 80 mM | 0.0372 mL | 0.1858 mL | 0.3716 mL | 0.9289 mL | |
| 100 mM | 0.0297 mL | 0.1486 mL | 0.2973 mL | 0.7431 mL |
GSK_WRN4 Related Classifications
HY-163942 Related Classifications
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