WX-02-23
Based on 1 Customer Validation
WX-02-23 is a small-molecule probe that stereoselectively and site-specifically binds to C258 of FOXA1 and C1111 of SF3B1. WX-02-23 remodels FOXA1's chromatin binding and pioneer activity in a DNA-dependent manner, disrupts spliceosome assembly, and enhances the thermal stability of SF3B1. WX-02-23 inhibits tumor cell proliferation and induces apoptosis. WX-02-23 can be used for research on cancers such as prostate cancer.
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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 : 99.88%
- CAS 番号: 2929223-35-6
- 分子式: C26H25N3O5
- 分子量:459.49
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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
生物活性
製品説明
IC50 & Target
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FOXA1 |
体外実験
WX-02-23 (20 µM; 3 h) binds to FOXA1_C258 in a stereoselective and site-specific manner in 22Rv1 prostate cancer cells[1].
WX-02-23 (20 μM; 2 h) stereoselectively inhibits CJR-6A-mediated enrichment of FOXA1 in 22Rv1 prostate cancer cells (IC50 = 5.5 μM)[1].
WX-02-23 (20 µM; 3 h) remodels FOXA1 binding and chromatin accessibility in 22Rv1 prostate cancer cells[1].
WX-02-23 (200 µM; 10 min) increases the thermal stability of SF3B1 in nuclear extracts NE-3 from HeLa cells[3].
WX-02-23 (0.2–200 µM; 60 min) inhibits the splicing of precursor mRNA in HeLa cell nuclear extracts, with an IC50 of approximately 5 µM[3].
WX-02-23 (0.1-100 μM; 24-72 h) inhibits proliferation of 22Rv1 cells (IC50 = 170 nM) and induces apoptosis in THP1 cells, among others[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Parental and C1111S-SF3B1 22Rv1 human prostate cancer cells
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Concentration:0.01-100 μM
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Incubation Time:72 h
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Result:Inhibited the growth of parental 22Rv1 cells with a GI50 of 9.5 μM (95% confidence interval: 9.0-10.1 μM).
Inhibited the growth of C1111S-SF3B1 22Rv1 cells with a GI50 of 12.2 μM (95% confidence interval: 11.0-13.6 μM).
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Cell Line:22Rv1 human prostate cancer cells
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Concentration:dose range
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Incubation Time:72 h
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Result:Exhibited minimal anti-proliferative activity, with significantly reduced potency compared to its active enantiomer WX-02-23 (IC50 not reported, as it was the inactive stereoisomer).
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Somatic Cell Culture
- CFSE Dye Dilution Proliferation Assay
- Dye-dilution cell tracking and proliferation staining
- CCK-8/WST-8 Cell Proliferation Assay
- Protocol for Cell Cycle
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Cell Viability Determination by MTT Colorimetric Assay
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Ki-67 Immunostaining Proliferation Assay
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- PCNA Immunodetection Proliferation Assay
- Protocol for Cell Counting and Cell Density Analysis
- Apoptosis Solutions
- MTT Cell Proliferation Assay
化学情報
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CAS 番号 2929223-35-6
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性状 Solid
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分子量 459.49
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分子式 C26H25N3O5
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Color Light yellow to yellow
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SMILES
O=C(C=C)N([C@H](C(N1CCOCC1)=O)C2)[C@H](C3=CC=C(OCO4)C4=C3)C5=C2C6=C(N5)C=CC=C6
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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 : 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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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.
Working solution concentration: 0.22 mg/mL
純度とドキュメンテーション
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データシート (283 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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取扱説明書 (2659 KB)
参考文献
[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]
[2]. Khan KS, et al. A small molecule that reshapes the chromatin dynamics of FOXA1. Mol Cell. 2024;84(21):4049-4051. [Content Brief]
[3]. Amorello AN, et al. SF3B1 thermostability as an assay for splicing inhibitor interactions. J Biol Chem. 2025;301(2):108135. [Content Brief]
[4]. 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 |
WX-02-23 関連分類
HY-168534 関連分類
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