MS181
Based on 1 Customer Validation
MS181 (compound 1) is a potent cereblon (CRBN)-recruiting and EED-binding polycomb repressive complex 1 (PRC1) PROTAC degrader. MS181 decreases the expression of EED, EZH2, SUZ12, BMI1 and RING1B. MS181 shows antiproliferative activity (Strtucture Note: Red, EED binder (HY-158771); Blue, CRBN ligand (HY-41547); Black, Linker HY-131717).
(Pink: E1/E2/E3 Enzyme ligand (HY-158771); Blue: Cereblon ligand (HY-41547); Black: linker).
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: 98.36%
- CAS 番号: 3037165-65-1
- 分子式: C39H41N11O6
- 分子量:759.81
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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
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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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生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| K562 | GI50 |
3.7 μM
Compound: 1; MS181
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Antiproliferative activity against human K562 cells assessed as cell growth inhibition incubated for 7 days by WST-8 assay
Antiproliferative activity against human K562 cells assessed as cell growth inhibition incubated for 7 days by WST-8 assay
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[PMID: 38607318] |
MS181 (compound 1) (0, 0.1, 0.3, 1, 3, 10 µM; 24 h) decreases the expression of EED, EZH2, SUZ12, BMI1 and RING1B in a dose dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:K562 cells
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Concentration:0, 0.1, 0.3, 1, 3, 10 µM
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Incubation Time:24 h
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Result:Decreassed the expression of EED, EZH2, SUZ12, BMI1 and RING1B, H3K27me3 in a dose dependent manner, showed no changes in the histone H3 lysine 27 trimethylation (H3K27me3) mark catalyzed by the PRC2 complex.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male swiss albino mice[1]
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Dosage:50 mg/kg
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Administration:I.p.; once
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Result:Showed above 1 μM for the first 2 h and maintained above 0.50 μM for 8 h post in the plasma concentration.
化学情報
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CAS 番号 3037165-65-1
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性状 Solid
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分子量 759.81
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分子式 C39H41N11O6
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Color Light yellow to yellow
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SMILES
O=C(NCCCCN1CCN(C2=CC=C(C3=CN=C(N4C3=NN=C4)NCC5=CC=CO5)C=C2)CC1)CNC6=CC=CC(C(N7C8C(NC(CC8)=O)=O)=O)=C6C7=O
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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 : 100 mg/mL (131.61 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 (271 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 | 1.3161 mL | 6.5806 mL | 13.1612 mL | 32.9030 mL |
| 5 mM | 0.2632 mL | 1.3161 mL | 2.6322 mL | 6.5806 mL | |
| 10 mM | 0.1316 mL | 0.6581 mL | 1.3161 mL | 3.2903 mL | |
| 15 mM | 0.0877 mL | 0.4387 mL | 0.8774 mL | 2.1935 mL | |
| 20 mM | 0.0658 mL | 0.3290 mL | 0.6581 mL | 1.6451 mL | |
| 25 mM | 0.0526 mL | 0.2632 mL | 0.5264 mL | 1.3161 mL | |
| 30 mM | 0.0439 mL | 0.2194 mL | 0.4387 mL | 1.0968 mL | |
| 40 mM | 0.0329 mL | 0.1645 mL | 0.3290 mL | 0.8226 mL | |
| 50 mM | 0.0263 mL | 0.1316 mL | 0.2632 mL | 0.6581 mL | |
| 60 mM | 0.0219 mL | 0.1097 mL | 0.2194 mL | 0.5484 mL | |
| 80 mM | 0.0165 mL | 0.0823 mL | 0.1645 mL | 0.4113 mL | |
| 100 mM | 0.0132 mL | 0.0658 mL | 0.1316 mL | 0.3290 mL |
MS181 関連分類
HY-158239 関連分類
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