MU147
Based on 1 Customer Validation
MU147 is an MRE11 nuclease inhibitor and chemical probe with anticancer activity, exhibiting IC50 values of 3.7 μM and 0.8 μM against the nuclease activity of human MRE11 and the MRN complex, respectively. MU147 inhibits MRE11 exonuclease and endonuclease activities, preventing MRN-dependent DNA end resection and nascent DNA degradation at stalled replication forks in BRCA2-deficient cells. MU147 delays the DNA damage repair process, inhibits homologous recombination and alternative non-homologous end joining, downregulates ionizing radiation- or camptothecin-induced RPA/RPA32 phosphorylation, and reduces survival of BRCA2-deficient cells. MU147 directly binds MRE11 in cells and impairs its recruitment to damage foci. MU147 can be used in cancer-related research.
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- 純度 : 99.35%
- CAS 番号: 2379405-61-3
- 分子式: C19H13N3O3S
- 分子量:363.39
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
生物活性
製品説明
IC50 & Target
MRE11[1]
体外実験
MU147 (25 μM; 72 h) inhibits MRE11-dependent HR and A-NHEJ double-strand break repair in U2OS and HEK-293T reporter cells[1].
MU147 (25-50 μM) inhibits DNA end resection and RPA32 S4/S8 phosphorylation in CPT (HY-16560)-exposed U2OS cells, with an IC50 of 19 μM for RPA32 pS4/S8 foci, and reduces pRPA S4/S8 and γH2AX immunoblot signals[1].
MU147 (25 μM; co-exposure with 4 mM HU (HY-B0313) for 4 hours) rescues nascent DNA degradation at stalled replication forks in BRCA2-deficient DLD1 cells[1].
MU147 (100 μM; 60 minutes) does not directly bind FEN1 in U2OS cells under CETSA conditions[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U2OS, DLD1, and isogenic BRCA2-proficient/deficient DLD1 cells
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Concentration:25 μM
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Incubation Time:72 h
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Result:U2OS cells exhibited minimal sensitivity to MU147, whereas proliferation of DLD1 cells was impaired.
Significantly reduced survival of BRCA2-deficient DLD1 cells.
Had minimal effects on cell-cycle distribution in U2OS cells.
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Cell Line:U2OS cells
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Concentration:25 and 50 μM
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Incubation Time:pre-treated with
indicated concentrations of the inhibitors for 30 min, followed by treatment with CPT (1 μM) for 1 h -
Result:Reduced pRPA S4/S8 and γH2AX immunoblot signals.
化学情報
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CAS 番号 2379405-61-3
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性状 Solid
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分子量 363.39
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分子式 C19H13N3O3S
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Color Light yellow to yellow
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SMILES
OC1=CC(/C=C(C#N)/C(NC2=NC(C3=CC=CC=C3)=CS2)=O)=CC=C1O
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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 In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
体外:
DMSO : 116.67 mg/mL (321.06 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)
純度とドキュメンテーション
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データシート (277 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
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 | 2.7519 mL | 13.7593 mL | 27.5186 mL | 68.7966 mL |
| 5 mM | 0.5504 mL | 2.7519 mL | 5.5037 mL | 13.7593 mL | |
| 10 mM | 0.2752 mL | 1.3759 mL | 2.7519 mL | 6.8797 mL | |
| 15 mM | 0.1835 mL | 0.9173 mL | 1.8346 mL | 4.5864 mL | |
| 20 mM | 0.1376 mL | 0.6880 mL | 1.3759 mL | 3.4398 mL | |
| 25 mM | 0.1101 mL | 0.5504 mL | 1.1007 mL | 2.7519 mL | |
| 30 mM | 0.0917 mL | 0.4586 mL | 0.9173 mL | 2.2932 mL | |
| 40 mM | 0.0688 mL | 0.3440 mL | 0.6880 mL | 1.7199 mL | |
| 50 mM | 0.0550 mL | 0.2752 mL | 0.5504 mL | 1.3759 mL | |
| 60 mM | 0.0459 mL | 0.2293 mL | 0.4586 mL | 1.1466 mL | |
| 80 mM | 0.0344 mL | 0.1720 mL | 0.3440 mL | 0.8600 mL | |
| 100 mM | 0.0275 mL | 0.1376 mL | 0.2752 mL | 0.6880 mL |