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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.83%
- CAS. Nr.: 3107482-42-5
- Formel: C21H22N6O2S
- Molecular Weight:422.50
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Speicherung: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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
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Biologische Aktivität
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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.
Chemical Information
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CAS. Nr. 3107482-42-5
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Appearance Solid
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Molecular Weight 422.50
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (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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Handling Instructions (2659 KB)
Verweise
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 Related Classifications
HY-173002 Related Classifications
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