WX2-43
Based on 1 Customer Validation
WX2-43 is a PRMT5-KLF4 inhibitor (Kd of 11.0 nM). WX2-43 binds to the region between amino acids L400-M500 on PRMT5. WX2-43 efficiently intercepts the interaction between KLF4 and PRMT5, and blocks KLF4 methylation. WX2-43 decreases p21 levels and increases Bax levels. WX2-43 suppresses triple negative breast tumor progression. WX2-43 can be used in the research of triple-negative breast cancer and colorectal cancer.
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- Pureza: 98.74%
- No. CAS: 723754-14-1
- Fòrmula: C17H21ClN2
- Peso molecular:288.82
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Chemical Information
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Solvente y solubilidad
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Actividad biológica
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PRMT5 11.0 nM (Kd) |
Bax |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCC1937 | EC50 |
0.44 μM
Compound: 84; WX2-43
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Anticancer activity against human HCC1937 cells assessed as cell growth inhibition
Anticancer activity against human HCC1937 cells assessed as cell growth inhibition
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[PMID: 33650861] |
| HCC38 | EC50 |
1.2 μM
Compound: 84; WX2-43
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Anticancer activity against human HCC38 cells assessed as cell growth inhibition
Anticancer activity against human HCC38 cells assessed as cell growth inhibition
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[PMID: 33650861] |
| MCF7 | EC50 |
0.77 μM
Compound: 84; WX2-43
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Anticancer activity against human MCF7 cells assessed as cell growth inhibition
Anticancer activity against human MCF7 cells assessed as cell growth inhibition
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[PMID: 33650861] |
| MDA-MB-453 | EC50 |
2.51 μM
Compound: 84; WX2-43
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Anticancer activity against human MDA-MB-453 cells assessed as cell growth inhibition
Anticancer activity against human MDA-MB-453 cells assessed as cell growth inhibition
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[PMID: 33650861] |
| MDA-MB-468 | EC50 |
2.5 μM
Compound: 84; WX2-43
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Anticancer activity against human MDA-MB-468 cells assessed as cell growth inhibition
Anticancer activity against human MDA-MB-468 cells assessed as cell growth inhibition
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[PMID: 33650861] |
WX2-43 (biotin-WX2-43; 0.1 nM-10 μM; 2 h) binds to PRMT5 with a Kd of 11.0 nM[1].
WX2-43 (0.03-10 μM; 24 h) inhibits cell viability in a KLF4-dependent manner in MEFs treated with cisplatin[1].
WX2-43 is more potent in TNBC cell lines (EC50 0.44-0.96 μM) than in normal mammary epithelial cell lines (EC50 3.62-23.34 μM)[1].
WX2-43 can induce a mesenchymal-like phenotype in two-dimensional (2D) AKPS cultures, altering colony morphology, size, and actin cytoskeleton, and reducing the frequency of Ki-67+ cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:KLF4+/+ MEFs, KLF4-/- MEFs
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Concentration:0, 0.03, 0.1, 0.3, 1, 3, 10 μM (WX2-43); 5 μM (cisplatin)
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Incubation Time:24 h
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Result:Reduced viability in KLF4+/+ MEFs in a dose-dependent manner; showed no effect on viability in KLF4-/- MEFs.
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Cell Line:MDA-MB-231
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Concentration:0, 0.1, 1, 10 μM
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Incubation Time:24 h
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Result:Decreased KLF4 protein levels and p21 levels and increased Bax levels in a dose-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Crl: Nu-Foxn1(nu) (female, 8 weeks old)[1]
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Dosage:40 mg/kg; 80 mg/kg
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Administration:i.p.; twice weekly; 4 weeks
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Result:Reduced tumor size and weight by approximately 40% at 40 mg/kg compared to vehicle; Reduced tumor size and weight by approximately 60% at 80 mg/kg compared to vehicle; Confirmed reduced KLF4 protein levels in treated groups via western blotting.
Chemical Information
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No. CAS 723754-14-1
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Appearance Solid
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Peso molecular 288.82
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Fòrmula C17H21ClN2
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Color White to off-white
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SMILES
ClC1=CC=C(C=C1)NCC2=CC=C(C=C2)N(CC)CC
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : ≥ 100 mg/mL (346.24 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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)
Pureza y Documentación
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Ficha de datos (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
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- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Zhou Z, et al. A novel small-molecule antagonizes PRMT5-mediated KLF4 methylation for targeted therapy. EBioMedicine. 2019;44:98-111. [Content Brief]
[2]. Borrelli C, et al. In vivo interaction screening reveals liver-derived constraints to metastasis. Nature. 2024;632(8024):411-418. [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 | 3.4624 mL | 17.3118 mL | 34.6236 mL | 86.5591 mL |
| 5 mM | 0.6925 mL | 3.4624 mL | 6.9247 mL | 17.3118 mL | |
| 10 mM | 0.3462 mL | 1.7312 mL | 3.4624 mL | 8.6559 mL | |
| 15 mM | 0.2308 mL | 1.1541 mL | 2.3082 mL | 5.7706 mL | |
| 20 mM | 0.1731 mL | 0.8656 mL | 1.7312 mL | 4.3280 mL | |
| 25 mM | 0.1385 mL | 0.6925 mL | 1.3849 mL | 3.4624 mL | |
| 30 mM | 0.1154 mL | 0.5771 mL | 1.1541 mL | 2.8853 mL | |
| 40 mM | 0.0866 mL | 0.4328 mL | 0.8656 mL | 2.1640 mL | |
| 50 mM | 0.0692 mL | 0.3462 mL | 0.6925 mL | 1.7312 mL | |
| 60 mM | 0.0577 mL | 0.2885 mL | 0.5771 mL | 1.4427 mL | |
| 80 mM | 0.0433 mL | 0.2164 mL | 0.4328 mL | 1.0820 mL | |
| 100 mM | 0.0346 mL | 0.1731 mL | 0.3462 mL | 0.8656 mL |
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