WSB1 Degrader 1
Based on 1 Customer Validation
WSB1 Degrader 1 is an orally active WSB1 degrader that inhibits cancer cell migration. WSB1 Degrader 1 induces time- and concentration-dependent degradation of WSB1 in a proteasome-dependent manner, increases RhoGDI2 protein levels, and reduces WSB1-driven F-actin organization and membrane ruffling. WSB1 Degrader 1 can be used in studies of cancer metastasis.
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- Pureté: 99.81%
- CAS No.: 2306039-66-5
- Formule: C21H22N2O2
- Masse moléculaire:334.41
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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
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
WSB1 |
In Vitro
WSB1 Degrader 1 (compound 4) (5 μM; 16 h) inhibits migration of KHOS osteosarcoma cells, with a normalized migration rate of 0.51, and exhibits a cytotoxic IC50 of 39.1 μM against KHOS cells[1].
WSB1 Degrader 1 (10 μM; 48 h) inhibits migration of H460 non-small cell lung cancer cells with a normalized migration rate of 0.48, and exhibits a cytotoxic IC50 of 24.47 μM against H460 cells[1].
WSB1 Degrader 1 (5 μM) inhibits the migration of KHOS osteosarcoma cells under both normoxic and hypoxic conditions, with normalized migration rates of 0.54 and 0.82, respectively[1].
WSB1 Degrader 1 inhibits the migration of KHOS osteosarcoma cells with overexpressed WSB1, with a normalized migration rate of 0.31[1].
WSB1 Degrader inhibits the migration of H1299 non-small cell lung cancer cells with overexpressed WSB1[1].
WSB1 Degrader 1 inhibits migration of wild-type A2780 ovarian cancer cells, but does not affect migration of WSB1-knockout A2780 cells, indicating that it exerts WSB1-dependent activity[1].
WSB1 Degrader 1 reduces Myc-WSB1 and Flag-WSB1 protein levels and increases RhoGDI2 protein levels in H1299-WSB1 cells; MG132, but not Chloroquine, blocks WSB1 degradation, supporting that it induces WSB1 degradation in a proteasome-dependent manner[1].
WSB1 Degrader 1 (20 μM; 2-24 h) reduces WSB1 protein levels in H1299-WSB1 cells in a time-dependent manner; in concentration gradient assays, WSB1 protein levels decrease with exposure to WSB1 Degrader 1, whereas no corresponding reduction is observed for Flag-GFP[1].
WSB1 Degrader 1 does not alter the mRNA levels of WSB1 and RhoGDI2 in H1299-WSB1 cells, indicating that the protein changes it induces are not caused by reductions in the corresponding mRNA levels[1].
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WSB1 Degrader 1 (20 μM; 24 h) reduces F-actin fluorescence intensity and membrane ruffling in H1299-WSB1 cells, thereby reversing the WSB1-driven cytoskeletal remodeling phenotype[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:KHOS osteosarcoma cells
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Concentration:5 μM
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Incubation Time:16 h
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Result:Inhibited KHOS cell migration, resulting in a normalized migration rate of 0.51.
Exhibited a cytotoxic IC50 of 39.1 μM against KHOS cells.
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Cell Line:H460 non-small-cell lung cancer cells
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Concentration:10 μM
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Incubation Time:48 h
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Result:Inhibited H460 cell migration, resulting in a normalized migration rate of 0.40.
Resulted in a normalized migration rate of 0.48 at 10 μM.
Exhibited a cytotoxic IC50 of 24.47 μM against H460 cells.
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Cell Line:WSB1-overexpressing KHOS osteosarcoma cells (KHOS-WSB1), empty plasmid-transduced KHOS cells (KHOS-pCDH)
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Concentration:5 μM
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Incubation Time:24 h
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Result:Blocked WSB1-enhanced wound healing in KHOS-WSB1 cells, resulting in a normalized migration rate of 0.31.
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Cell Line:H1299-WSB1 non-small-cell lung cancer cells
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Concentration:20 μM
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Incubation Time:24 h
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Result:Reduced fluorescence intensity of F-actin and decreased formation of membrane ruffles, reversing the WSB1-driven enhancement of F-actin expression and membrane ruffle formation.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/c (nu/nu) nude mice (implanted with highly metastatic 4T1 breast cancer cells)[1]
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Dosage:100 mg/kg
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Administration:p.o.; daily; 28 days
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Result:Reduced the average number of lung metastatic colonies from 14.3 in untreated controls to 5.7.
Chemical Information
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CAS No. 2306039-66-5
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Appearance Solid
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Masse moléculaire 334.41
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Formule C21H22N2O2
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Color Off-white to light yellow
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SMILES
NC1=NC(C2=CC=C(OC)C(C)=C2)=C(C3=CC=C(OC)C(C)=C3)C=C1
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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 : 25 mg/mL (74.76 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: ≥ 2.08 mg/mL (6.22 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 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.
Pureté et documentation
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Fiche technique (293 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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 | 2.9903 mL | 14.9517 mL | 29.9034 mL | 74.7585 mL |
| 5 mM | 0.5981 mL | 2.9903 mL | 5.9807 mL | 14.9517 mL | |
| 10 mM | 0.2990 mL | 1.4952 mL | 2.9903 mL | 7.4759 mL | |
| 15 mM | 0.1994 mL | 0.9968 mL | 1.9936 mL | 4.9839 mL | |
| 20 mM | 0.1495 mL | 0.7476 mL | 1.4952 mL | 3.7379 mL | |
| 25 mM | 0.1196 mL | 0.5981 mL | 1.1961 mL | 2.9903 mL | |
| 30 mM | 0.0997 mL | 0.4984 mL | 0.9968 mL | 2.4920 mL | |
| 40 mM | 0.0748 mL | 0.3738 mL | 0.7476 mL | 1.8690 mL | |
| 50 mM | 0.0598 mL | 0.2990 mL | 0.5981 mL | 1.4952 mL | |
| 60 mM | 0.0498 mL | 0.2492 mL | 0.4984 mL | 1.2460 mL |
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