MS181
Based on 1 Customer Validation
MS181 is a BMI1 and RING1B degrader with antiproliferative activity. MS181 induces degradation via an EED-, CRBN-, and ubiquitin-proteosome system-dependent pathway, with preferential targeting over PRC2 components. MS181 acts in VHL-defective cancer cells. MS181 serves as a chemical biology tool to study PRC1 roles in cancer. MS181 can be used for the research of myelogenous leukemia, renal cell carcinoma, metastatic prostate cancer, triple negative breast cancer.
(Pink: E1/E2/E3 Enzyme ligand (HY-158771); Blue: Cereblon ligand (HY-41547); Black: linker).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.36%
- No. CAS: 3037165-65-1
- Fòrmula: C39H41N11O6
- Peso molecular:759.81
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
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Cereblon |
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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 binds to the purified recombinant C-terminal domain (75-441) of EED with a KD value of 190 nM[1].
MS181 (up to 15 μM) does not inhibit the growth of normal prostate PNT2 cells at concentrations as high as 15 μM[1].
MS181 (0-10 μM; 24 h) preferentially degrades canonical PRC1 components BMI1 (DC50 = 1.7 μM) and RING1B (DC50 = 1.3 μM), rather than EED (DC50 = 3.3 μM), in K562 cells in an EED-, CRBN- and ubiquitin-proteasome system-dependent manner[1].
MS181 inhibits the proliferation of K562 myeloid leukemia cells with a GI50 of 3.7 μM, and upregulates PRC1 target genes HoxA and HoxD by 3.1-fold and 2.3-fold, respectively[1].
MS181 (10-30 μM) degrades BMI1 and RING1B, reduces the H2AK119ub modification mark, and inhibits the proliferation of 786-O VHL-deficient renal cancer cells at concentrations of 15 μM and 30 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:K562 myelogenous leukemia cells
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Concentration:Various concentrations; 10 μM
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Incubation Time:24 h; 20-24 h; 4 h, 12 h
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Result:Preferentially degraded PRC1 components BMI1 and RING1B with DC50 values of 1.7 μM and 1.3 μM, respectively, while degrading EED with a DC50 of 3.3 μM.
Caused modest downregulation of EZH2 and SUZ12, significantly reduced the PRC1-catalyzed H2AK119ub mark, and did not alter the PRC2-catalyzed H3K27me3 mark.
Degradation of BMI1 and RING1B was detectable as early as 4 h and nearly complete by 12 h, while ~50% of EED remained at 12 h.
Did not degrade noncanonical PRC1 components RYBP, YAF, or CBX8 at up to 10 μM, but modestly degraded RING1A at 10 μM.
Pretreatment with EED226, pomalidomide, MLN4924, or MG132 rescued BMI1 and RING1B degradation induced by MS181.
Did not significantly alter mRNA levels of BMI1, RING1B, or EED.
| Species | Dose | Route | Plasma Concentration |
|---|---|---|---|
| Mice[1] | 50 mg/kg | i.p. | >1 (2 h) μM |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 3037165-65-1
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Appearance Solid
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Peso molecular 759.81
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
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)
Pureza y Documentación
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Ficha de datos (273 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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Instrucciones de manejo (2659 KB)
Referencias
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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