| Size | Price | Stock | Qty |
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| 1mg |
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| 100mg | |||
| Other Sizes |
| Targets |
MS0124 targets G9a-like protein (GLP), a protein lysine methyltransferase (PKMT). GLP and G9a share approximately 80% sequence identity in their catalytic domains and often form a heterodimer complex. They are responsible for the majority of H3K9 mono- and dimethylation, which is a hallmark of transcriptionally silent chromatin. By selectively inhibiting GLP, MS0124 allows researchers to study the specific role of this enzyme in gene silencing, independent of G9a.
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| ln Vitro |
In vitro, MS0124 demonstrates potent and selective inhibitory activity. It inhibits GLP with an IC₅₀ of 13 ± 4 nM. In contrast, its activity against G9a is significantly weaker, with an IC₅₀ of 440 ± 63 nM. This represents a 34-fold selectivity for GLP over G9a. The compound's high potency and selectivity make it an excellent chemical probe for studying the specific biological functions of GLP in epigenetic regulation.
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| ln Vivo |
In vivo data for MS0124 are not extensively reported in publicly available sources. As a potent and selective epigenetic inhibitor, it holds significant promise for in vivo studies to validate GLP as a therapeutic target in diseases where epigenetic dysregulation plays a role, such as cancer. Its ability to selectively modulate H3K9 methylation makes it a potential tool for investigating the role of this epigenetic mark in various disease models. Further studies are needed to characterize its in vivo efficacy and pharmacokinetic properties.
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| Enzyme Assay |
In vitro enzyme assays for MS0124 typically use recombinant GLP or G9a enzymes and a peptide substrate representing the histone H3 tail. The compound is dissolved in DMSO and serially diluted in assay buffer. The enzymatic reaction is initiated by the addition of the substrate and the methyl donor S-adenosylmethionine (SAM). After incubation, the extent of methylation is measured using methods such as scintillation proximity assay (SPA), AlphaLISA, or mass spectrometry. IC₅₀ values are calculated by fitting the dose-response data to a nonlinear regression model.
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| Cell Assay |
For cell-based assays, relevant cancer cell lines are cultured in standard media. Cells are seeded in multi-well plates and treated with MS0124 at various concentrations for a period of several days. Following treatment, the levels of histone H3K9 methylation (both mono- and dimethylation) are assessed by Western blotting or immunofluorescence using specific antibodies. The effects on gene expression can be analyzed by RNA-sequencing or RT-PCR. Cell viability and proliferation are measured using standard assays like MTT or CellTiter-Glo. All experiments include appropriate vehicle controls and are performed in triplicate.
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| Animal Protocol |
In vivo, MS0124 may be administered to rodents via intraperitoneal (IP) or oral routes for efficacy studies in disease models. The compound is formulated in a suitable vehicle. Dosing regimens would be determined based on preliminary pharmacokinetic and tolerability studies. Endpoints for efficacy studies could include measuring tumor growth inhibition in xenograft models, analyzing changes in global H3K9 methylation levels in tissues, and assessing the expression of GLP target genes. All procedures must be conducted in accordance with institutional animal care guidelines.
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| ADME/Pharmacokinetics |
Detailed pharmacokinetic properties of MS0124 are not extensively reported in public sources. The compound has a molecular weight of 387.48 and is soluble in DMSO. It is typically stored as a powder at -20°C. For in vivo applications, it would be formulated in a suitable vehicle to ensure adequate exposure. A comprehensive ADME profile is essential for interpreting results from in vivo studies and is a prerequisite for any potential therapeutic development.
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| Toxicity/Toxicokinetics |
Toxicological data for MS0124 are limited. As an inhibitor of a key epigenetic enzyme, its safety profile requires careful evaluation. The compound is for research use only and is not for human consumption. Potential toxicity could arise from on-target effects on gene expression. Comprehensive toxicology studies would be required for any future therapeutic application.
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| References |
: Discovery of Potent and Selective Inhibitors for
G9a-Like Protein (GLP) Lysine Methyltransferase. J Med Chem. 2017 Feb 14.
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| Additional Infomation |
MS0124 is a research-grade chemical probe, and its primary application is in the field of epigenetics, specifically for studying the role of GLP in gene regulation. Its high potency and selectivity make it an invaluable tool for dissecting the distinct functions of GLP and G9a. The compound is not an approved drug and has not entered clinical trials. It is commercially available from various chemical suppliers for research purposes only.
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| Molecular Formula |
C20H29N5O3
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|---|---|
| Molecular Weight |
387.475964307785
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| Exact Mass |
387.227
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| CAS # |
1197196-63-6
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| Related CAS # |
1197196-63-6;
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| PubChem CID |
44605026
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| Appearance |
White to off-white solid powder
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| LogP |
2.5
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
28
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| Complexity |
485
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN1CCC(CC1)NC2=NC(=NC3=CC(=C(C=C32)OC)OC)N4CCOCC4
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| InChi Key |
MEVMMQQJOXBSAX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H29N5O3/c1-24-6-4-14(5-7-24)21-19-15-12-17(26-2)18(27-3)13-16(15)22-20(23-19)25-8-10-28-11-9-25/h12-14H,4-11H2,1-3H3,(H,21,22,23)
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| Chemical Name |
6,7-dimethoxy-N-(1-methylpiperidin-4-yl)-2-morpholinoquinazolin-4-amine
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| Synonyms |
MS0124 MS 0124MS-0124
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5808 mL | 12.9039 mL | 25.8078 mL | |
| 5 mM | 0.5162 mL | 2.5808 mL | 5.1616 mL | |
| 10 mM | 0.2581 mL | 1.2904 mL | 2.5808 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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