MS9024
Based on 1 Customer Validation
MS9024 is a selective DNMT1 Molecular glue degrader with a DC50 of 35 nM. MS9024 degrades DNMT1 in a concentration-, time- and proteasome-dependent manner without altering DNMT1 transcription. MS9024 mediates degradation via HECT E3 ligase and/or UHRF1, but not via lysosomes or Cullin RING E3 ligase. MS9024 can be used in the research of colorectal cancer, breast cancer and non-small cell lung cancer.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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: 99.83%
- CAS 番号: 3107482-42-5
- 分子式: C21H22N6O2S
- 分子量:422.50
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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
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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Epigenetics Compound Library
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Anti-Cancer Compound Library
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Anti-Blood Cancer Compound Library
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Transcription Factor-Targeted Library
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Anti-Colorectal Cancer Compound Library
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Molecular Glue Compound Library
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Anti-Hematopathy Compound Library
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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Methylation Compound Library
HY-L203
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High-Throughput Bioactive Compound Library
HY-L205
DNA Methyltransferase アイソフォーム固有の製品をすべて表示
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生物活性
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DNMT1 35 nM (DC50) |
MS9024 (0.001-5 μM; 2-24 h) degrades DNMT1 in HCT116 colorectal cancer cells in a time- and concentration-dependent manner, with an optimized DC50 of 35 nM[1].
MS9024 (0.001-5 μM; 24 h) potently degrades DNMT1 in MDA-MB-468 breast cancer cells (DC50 = 254 nM) and NCI-H1299 non-small cell lung cancer cells (DC50 = 101 nM), without altering DNMT1 mRNA levels[1].
MS9024 (1 μM) exhibits high selectivity for DNMT1, with no significant inhibitory effect on 11 other methyltransferases (including DNMT3A and DNMT3B) at a concentration of 1 μM. It does not degrade DNMT3A or DNMT3B in HCT116 cells, and only downregulates DNMT1 in global proteomic analysis[1].
Treatment with MS9024 (up to 15 μM for 7 days) exerts no significant inhibitory effect on the growth of HCT116 colorectal cancer cells (up to 15 μM) or MDA-MB-468 breast cancer cells (up to 10 μM) after 7 days[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116 colorectal cancer cells
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Concentration:0.001-5 μM
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Incubation Time:2-24 h
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Result:Induced DNMT1 degradation in a time-dependent manner.
Achieved a refined DC50 of 35 nM.
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Cell Line:HCT116 colorectal cancer cells, MDA-MB-468 breast cancer cells
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Concentration:Serial 3-fold dilutions up to 15 μM (HCT116); serial 3-fold dilutions up to 10 μM (MDA-MB-468)
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Incubation Time:7 days
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Result:Did not significantly inhibit cell growth in either cell line, with less than 50% inhibition at the highest tested concentrations.
化学情報
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CAS 番号 3107482-42-5
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性状 Solid
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分子量 422.50
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分子式 C21H22N6O2S
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Color White to off-white
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SMILES
CCC1=C(C(SC(C2=CC=CC=C2)C(N)=O)=NC(N(CC(NC)=O)C)=C1C#N)C#N
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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
DMSO : 8.33 mg/mL (19.72 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 (278 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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 | 2.3669 mL | 11.8343 mL | 23.6686 mL | 59.1716 mL |
| 5 mM | 0.4734 mL | 2.3669 mL | 4.7337 mL | 11.8343 mL | |
| 10 mM | 0.2367 mL | 1.1834 mL | 2.3669 mL | 5.9172 mL | |
| 15 mM | 0.1578 mL | 0.7890 mL | 1.5779 mL | 3.9448 mL |
MS9024 関連分類
HY-173002 関連分類
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