MS147
Based on 1 Customer Validation
MS147 is a VHL-based PROTAC degrader of BMI1 and RING1B (polycomb repressive complex 1 core components). MS147 directly binds EED and VHL E3 ligase, recruiting the ligase to the EED-BMI1/RING1B complex to induce time-dependent, ubiquitination-mediated degradation of BMI1 and RING1B. MS147 reduces histone H2A Lys119 mono-ubiquitination without altering histone H3 Lys27 tri-methylation and inhibits cancer cells proliferation. MS147 can be used for the research of cancer, such as chronic myelogenous leukemia and b-cell lymphoma.
(Pink: BMI1 and RING1B ligand (HY-183634); Blue: VHL ligand (HY-125845); Black: linker).
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 98.31%
- 화학식: C54H70N12O6S
- 분자량:1015.28
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보관: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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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
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VHL |
MS147 binds purified EED C-terminal domain (75-441) protein with a Kd of 3.0 μM[1].
MS147 binds purified VCB complex protein with a Kd of 450 nM[1].
MS147 (5 μM; 3-12 h) preferentially degrades BMI1 and RING1B over EED in KARPAS-422 cells, with near-complete PRC1 component degradation by 12 h[1].
MS147 (5 μM; 2-24 h) preferentially degrades BMI1 and RING1B over EED, and reduces H2AK119ub without altering H3K27me3, in K562 cells when treated at 5 μM[1].
MS147 (0.5-10 μM; 24 h) concentration-dependently degrades BMI1 and RING1B, reduces H2AK119ub in K562 cells[1].
MS147 (5 μM; 24 h) degrades BMI1 and RING1B in K562 cells in an EED-, VHL-, and ubiquitination-dependent manner[1].
MS147 (5 μM; 24 h) does not alter mRNA expression levels of BMI1, RING1B, or EED in KARPAS-422 cells when treated at 5 μM for 24 h[1].
MS147 (40 μM; 3 h) promotes formation of a BMI1-RING1B-EED-MS147-VHL complex in K562 cell lysates when treated at 40 μM for 3 h[1].
MS147 (5 days) inhibits proliferation of K562 cells with a GI50 of 3.8 μM after 5 days of treatment[1].
MS147 (5 days) inhibits proliferation of MDA-MB-231 cells with a GI50 of 4.5 μM after 5 days of treatment[1].
MS147 (5 days) inhibits proliferation of NCI-H1299 cells with a GI50 of 6.8 μM after 5 days of treatment[1].
MS147 (0.2-5 μM; 48 h) preferentially degrades BMI1 and RING1B over PRC2 components, and reduces H2AK119ub without altering H3K27me3, in MDA-MB-231 and NCI-H1299 cells when treated for 48 h[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:KARPAS-422 B-cell lymphoma cells
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Concentration:5 μM
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Incubation Time:3, 6, 12 h
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Result:Induced effective degradation of BMI1 and RING1B as early as 6 h, with near-complete degradation by 12 h.
Caused only partial degradation of EED at 12 h, demonstrating preferential degradation of PRC1 components over EED.
Chemical Information
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Appearance Solid
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분자량 1015.28
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화학식 C54H70N12O6S
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Color White to off-white
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SMILES
O=C([C@H]1N(C([C@@H](NC(CCCCCCNC(CCCCN2CCN(C3=CC=C(C4=CN=C(NCC5=CC=CO5)N6C4=NN=C6)C=C3)CC2)=O)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC7=CC=C(C8=C(C)N=CS8)C=C7
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 100 mg/mL (98.49 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)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (2.46 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (2.46 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (272 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 |
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| DMSO | 1 mM | 0.9849 mL | 4.9247 mL | 9.8495 mL | 24.6237 mL |
| 5 mM | 0.1970 mL | 0.9849 mL | 1.9699 mL | 4.9247 mL | |
| 10 mM | 0.0985 mL | 0.4925 mL | 0.9849 mL | 2.4624 mL | |
| 15 mM | 0.0657 mL | 0.3283 mL | 0.6566 mL | 1.6416 mL | |
| 20 mM | 0.0492 mL | 0.2462 mL | 0.4925 mL | 1.2312 mL | |
| 25 mM | 0.0394 mL | 0.1970 mL | 0.3940 mL | 0.9849 mL | |
| 30 mM | 0.0328 mL | 0.1642 mL | 0.3283 mL | 0.8208 mL | |
| 40 mM | 0.0246 mL | 0.1231 mL | 0.2462 mL | 0.6156 mL | |
| 50 mM | 0.0197 mL | 0.0985 mL | 0.1970 mL | 0.4925 mL | |
| 60 mM | 0.0164 mL | 0.0821 mL | 0.1642 mL | 0.4104 mL | |
| 80 mM | 0.0123 mL | 0.0616 mL | 0.1231 mL | 0.3078 mL |
MS147 Related Classifications
HY-160924 Related Classifications
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