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).
For research use only. We do not sell to patients.
- Purity: 98.36%
- CAS No.: 3037165-65-1
- Formula: C39H41N11O6
- Molecular Weight:759.81
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Storage: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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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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.
Chemical Information
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CAS No. 3037165-65-1
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Appearance Solid
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Molecular Weight 759.81
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (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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Handling Instructions (2659 KB)
References
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 Related Classifications
HY-158239 Related Classifications
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