Art. -Nr.: HY-161759

MS152

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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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Reinheit: 99.36%
CAS. Nr.: 3107476-89-8
Formel: C₂₂H₃₁N₃O₃
Molecular Weight:385.50

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

MS152 Chemical Structure

CAS. Nr.: 3107476-89-8

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

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)

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen :

In Vitro

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.

Western Blot Analysis^[1]

Cell Line:

K562 human leukemia cells
Concentration:

50-5000 nM
Incubation Time:

48 h
Result:

Dose-dependently reduced cellular H3K9me2 levels, with an EC₅₀ of 60 nM, which is 5-fold more potent than UNC0642.

Western Blot Analysis^[1]

Cell Line:

Prader-Willi syndrome (PWS) patient-derived fibroblasts
Concentration:

4-8 μM
Incubation Time:

4 days
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.

In Vivo

MS152 (5 mg/kg; i.p.; daily; 7 days) reactivates maternally imprinted genes in the brain of m^Snrpn-EGFP/p⁺ mice with greater efficiency than UNC0642, while maintaining normal body weight gain^[1].
MS152 (2.5 mg/kg; i.p.; daily; 5 days) ameliorates perinatal lethality and growth retardation in m⁺/p^{ΔSnrpn-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 m^Snrpn-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⁺/p^{ΔSnrpn-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 Snord116^m+/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.

Animal Model:

C57BL/6J mice (male and female, juvenile, postnatal day 21-23, maternally imprinted Snrpn-EGFP reporter model, m^{Snrpn-EGFP}/p^{+})^[1]
Dosage:

5 mg/kg
Administration:

i.p.; daily; 7 days
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.

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]
Dosage:

2.5 mg/kg
Administration:

i.p.; daily; 5 days
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.

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]
Dosage:

10 mg/kg
Administration:

p.o.; daily; 5 days
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

CAS. Nr. 3107476-89-8
Appearance Solid
Molecular Weight 385.50
Formel C₂₂H₃₁N₃O₃
Color White to off-white
SMILES

COC1=CC2=C(C=C1OCCCN3CCCC3)N=C(N)C=C2C4CCOCC4
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5940 mL

12.9702 mL

25.9403 mL

5 mM

0.5188 mL

2.5940 mL

5.1881 mL

10 mM

0.2594 mL

1.2970 mL

2.5940 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.49 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Wang SE, et al. Newly developed oral bioavailable EHMT2 inhibitor as a potential epigenetic therapy for Prader-Willi syndrome. Molecular therapy : the journal of the American Society of Gene Therapy. 2024 Aug 07;32(8):2662-2675. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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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MS152

Epigenetics Compound Library

Histone Modification Research Compound Library

Reprogramming Compound Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

MS152

Epigenetics Compound Library

Histone Modification Research Compound Library

Reprogramming Compound Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

MS152 Related Classifications

HY-161759 Related Classifications