WX-02-43
Based on 1 Customer Validation
WX-02-43 is a weak covalent inhibitor of SF3B1, and is the (1S,3R) enantiomer of WX-02-23 (HY-168534). WX-02-43 cannot effectively covalently modify the C258 site in the DNA-binding domain of FOXA1, and its inhibitory activity against SF3B1 is also weaker than that of WX-02-23. WX-02-43 serves as a negative control probe that fails to remodel the chromatin binding pattern and transcriptional activity of FOXA1. WX-02-43 can be used in studies on cancers such as prostate cancer to verify the specific effects of WX-02-23 on FOXA1 and SF3B1 targets.
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- Pureté: 99.49%
- CAS No.: 2929223-36-7
- Formule: C26H25N3O5
- Masse moléculaire:459.49
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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
WX-02-43 (20 μM; 3 h) does not bind to FOXA1C258, remodel the chromatin binding of FOXA1, or alter chromatin accessibility in human prostate cancer cell line 22Rv1[1].
WX-02-43 (0.01-100 μM; 72 h) inhibits the growth of parental and C1111S-SF3B1 22Rv1 human prostate cancer cells with comparable potency, with GI50 values of 9.5 μM and 12.2 μM, respectively[1].
WX-02-43 exhibits 4-fold weaker antiproliferative activity than WX-02-23 (HY-181421) in human cells[2].
WX-02-43 (5 μM; 2 h) does not act on SF3B1 in a stereoselective manner in human prostate cancer cell line 22Rv1 under the tested conditions[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2929223-36-7
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Appearance Solid
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Masse moléculaire 459.49
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Formule C26H25N3O5
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Color White to light yellow
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SMILES
C=CC(N1[C@@H](C2=CC=C(OCO3)C3=C2)C4=C(C[C@@H]1C(N5CCOCC5)=O)C6=CC=CC=C6N4)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 50 mg/mL (108.82 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)
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 (5.44 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 (5.44 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.
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 (281 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)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Won SJ, et al. Redirecting the pioneering function of FOXA1 with covalent small molecules. Mol Cell. 2024;84(21):4125-4141.e10. [Content Brief]
[3]. Lazear MR, et al. Proteomic discovery of chemical probes that perturb protein complexes in human cells. Mol Cell. 2023;83(10):1725-1742.e12. [Content Brief]
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 | 2.1763 mL | 10.8816 mL | 21.7633 mL | 54.4081 mL |
| 5 mM | 0.4353 mL | 2.1763 mL | 4.3527 mL | 10.8816 mL | |
| 10 mM | 0.2176 mL | 1.0882 mL | 2.1763 mL | 5.4408 mL | |
| 15 mM | 0.1451 mL | 0.7254 mL | 1.4509 mL | 3.6272 mL | |
| 20 mM | 0.1088 mL | 0.5441 mL | 1.0882 mL | 2.7204 mL | |
| 25 mM | 0.0871 mL | 0.4353 mL | 0.8705 mL | 2.1763 mL | |
| 30 mM | 0.0725 mL | 0.3627 mL | 0.7254 mL | 1.8136 mL | |
| 40 mM | 0.0544 mL | 0.2720 mL | 0.5441 mL | 1.3602 mL | |
| 50 mM | 0.0435 mL | 0.2176 mL | 0.4353 mL | 1.0882 mL | |
| 60 mM | 0.0363 mL | 0.1814 mL | 0.3627 mL | 0.9068 mL | |
| 80 mM | 0.0272 mL | 0.1360 mL | 0.2720 mL | 0.6801 mL | |
| 100 mM | 0.0218 mL | 0.1088 mL | 0.2176 mL | 0.5441 mL |
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