MS152
Based on 1 Customer Validation
MS152 is an orally active, blood-brain barrier penetrant inhibitor of EHMT2/G9a and EHMT1/GLP, with IC50s of 76 nM and 126 nM, repsectively. MS152 reduces H3K9me2 levels and reactivates maternally silenced Prader-Willi syndrome (PWS) genes. MS152 significantly improves perinatal lethality and growth retardation in mouse models, and is applicable to research related to Prader-Willi syndrome.
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- Purity: 99.36%
- CAS No.: 3107476-89-8
- 화학식: C22H31N3O3
- 분자량:385.50
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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
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Bioactive Compound Library Max
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MCE Bioactive Compound Library
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Bioactive Compound Library
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Methylation Compound Library
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High-Throughput Bioactive Compound Library
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Posttranslational Modification Library
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All Histone Methyltransferase Isoforms
More
Biological Activity
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EHMT1/GLP/KMT1D 76 nM (IC50) |
EHMT2/G9a/KMT1C 126 nM (IC50) |
EHMT1/GLP/KMT1D 6.2 nM (Kd) |
EHMT2/G9a/KMT1C 14.9 nM (Kd) |
MS152 (50-5000 nM; 48 h) dose-dependently reduces H3K9me2 levels in K562 cells with an EC50 of 60 nM[1].
MS152 (4-8 μM; 4 days) reduces H3K9me2 levels and potently reactivates maternally imprinted PWS-associated genes SNRPN, SNORD116, and IPW in PWS patient-derived fibroblasts at 4 μM and 8 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 human leukemia cells
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Concentration:50-5000 nM
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Incubation Time:48 h
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Result:Dose-dependently reduced cellular H3K9me2 levels, with an EC50 of 60 nM, which is 5-fold more potent than UNC0642.
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Cell Line:Prader-Willi syndrome (PWS) patient-derived fibroblasts
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Concentration:4-8 μM
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Incubation Time:4 days
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Result:Reduced H3K9me2 levels similarly to UNC0642 at 4 μM.
Reactivated expression of maternally imprinted PWS-associated genes SNRPN, SNORD116, and IPW more potently than UNC0642 at 4 μM and 8 μM.
Reduced H3K9me2 enrichment at the PWS-IC at 8 μM.
MS152 (2.5 mg/kg; i.p.; daily; 5 days) ameliorates perinatal lethality and growth retardation in m+/pΔSnrpn-Ube3a PWS mice, with sustained reactivation of maternally imprinted genes for up to 80 days post-treatment[1].
MS152 (50 mg/kg; p.o.; daily; 4 days) efficiently reactivates maternally imprinted genes in the brain of mSnrpn-EGFP/p+ mice while maintaining normal body weight gain[1].
MS152 (10 mg/kg; p.o.; daily; 5 days) ameliorates perinatal lethality and growth retardation in m+/pΔSnrpn-Ube3a PWS mice, with reactivation of maternally imprinted genes and no long-term effects on body weight or food consumption[1].
MS152 (2.5 mg/kg; i.p.; daily; 5 days) reactivates maternally imprinted Snord116 in the brain of Snord116m+/p- PWS mice while maintaining normal body weight gain[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J mice (male and female, juvenile, postnatal day 21-23, maternally imprinted Snrpn-EGFP reporter model, m^{Snrpn-EGFP}/p^{+})[1]
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Dosage:5 mg/kg
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Administration:i.p.; daily; 7 days
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Result:Significantly decreased neocortical H3K9me2 levels relative to vehicle treatment.
Reactivated expression of Snrpn-EGFP from the maternal chromosome more efficiently than UNC0642.
Caused no significant changes in body weight relative to vehicle-treated mice.
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Animal Model:C57BL/6J and 129SvEv mixed background mice (male and female, newborn, postnatal day 7-11, paternal deletion from Snrpn to Ube3a model, m^{+}/p^{ΔSnrpn-Ube3a})[1]
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Dosage:2.5 mg/kg
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Administration:i.p.; daily; 5 days
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Result:Prolonged survival of m^{+}/p^{ΔSnrpn-Ube3a} pups relative to vehicle-treated mice.
Significantly improved weight gain by postnatal day 25.
Maintained reactivation of maternally imprinted genes including Snurf-Snrpn, Snord116, and Snhg14 in forebrain and liver tissue at postnatal days 60 and 90.
Induced higher Snurf-Snrpn expression in male mice than females at postnatal day 90.
Caused no adverse effects on body weight or survival in wild-type mice treated with MS152.
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Animal Model:C57BL/6J and 129SvEv mixed background mice (male and female, newborn, postnatal day 4-8, paternal deletion from Snrpn to Ube3a model, m^{+}/p^{ΔSnrpn-Ube3a})[1]
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Dosage:10 mg/kg
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Administration:p.o.; daily; 5 days
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Result:Improved survival of m^{+}/p^{ΔSnrpn-Ube3a} pups relative to vehicle-treated mice.
Significantly improved weight gain by postnatal day 25.
Detected reactivation of maternally imprinted Snurf and Snord116 in forebrain and liver tissue at postnatal day 9.
Caused a slight decrease in forebrain H3K9me2 levels relative to vehicle treatment.
Caused no adverse effects on body weight in wild-type mice treated with MS152.
Maintained body weight and normalized food consumption comparable to controls at 8 months of age.
Chemical Information
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CAS No. 3107476-89-8
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Appearance Solid
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분자량 385.50
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화학식 C22H31N3O3
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Color White to off-white
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SMILES
COC1=CC2=C(C=C1OCCCN3CCCC3)N=C(N)C=C2C4CCOCC4
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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 : 50 mg/mL (129.70 mM; ultrasonic and warming and heat to 60°C; 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 (6.49 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 (6.49 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 (279 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)
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 | 2.5940 mL | 12.9702 mL | 25.9403 mL | 64.8508 mL |
| 5 mM | 0.5188 mL | 2.5940 mL | 5.1881 mL | 12.9702 mL | |
| 10 mM | 0.2594 mL | 1.2970 mL | 2.5940 mL | 6.4851 mL | |
| 15 mM | 0.1729 mL | 0.8647 mL | 1.7294 mL | 4.3234 mL | |
| 20 mM | 0.1297 mL | 0.6485 mL | 1.2970 mL | 3.2425 mL | |
| 25 mM | 0.1038 mL | 0.5188 mL | 1.0376 mL | 2.5940 mL | |
| 30 mM | 0.0865 mL | 0.4323 mL | 0.8647 mL | 2.1617 mL | |
| 40 mM | 0.0649 mL | 0.3243 mL | 0.6485 mL | 1.6213 mL | |
| 50 mM | 0.0519 mL | 0.2594 mL | 0.5188 mL | 1.2970 mL | |
| 60 mM | 0.0432 mL | 0.2162 mL | 0.4323 mL | 1.0808 mL | |
| 80 mM | 0.0324 mL | 0.1621 mL | 0.3243 mL | 0.8106 mL | |
| 100 mM | 0.0259 mL | 0.1297 mL | 0.2594 mL | 0.6485 mL |
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