M190S
Based on 1 Customer Validation
M109S is a novel small molecule protecting cells from mitochondria-dependent apoptosis both in vitro and in vivo. M109S has the potential to become a research tool for studying cell death mechanisms and to develop therapeutics targeting mitochondria-dependent cell death pathway. M109S has orally bioactivity with excellent brain permeability.
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- Pureté : 99.65%
- CAS No.: 2578300-07-7
- Formule: C21H21N5O2
- Masse moléculaire:375.42
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Stockage: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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
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caspase-3 23.4 nM (EC50) |
Caspase 3 23.4 nM (EC50) |
In Vitro
M109S (0.1-10000 nM, 24-48 h) inhibits apoptosis induced by Bax as well as Bak[1].
M109S (0-10μM, 4 h) suppresses Staurosporine (HY-15141 STS)-induced apoptosis in MEFs [1].
M109S (0-10μM, 24 h) inhibits Etoposide (HY-13629)-induced apoptosis in Neuro2a cells[1].
M109S (500 nM, 24 h) inhibits Obatoclax (HY-10969A)-induced apoptosis in ARPE19 cells[1].
M109S (500 nM, 48 h) suppresses the conformation change (N-terminal exposure) and mitochondrial translocation of Bax[1].
M109S (1.0 μM, 4h) decreases mitochondrial oxygen consumption and reactive oxygen species, whereas M109S (0.1-1 nM, 4 h) increases glycolysis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:MEF(Wt, Bax only, Bak only)
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Concentration:0.1 nM, 1 nM, 10 nM, 100 nM, 10000 nM
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Incubation Time:24 h((WT and Bax-only), 48 h (Bak-only)
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Result:Showed a dose-dependent suppression of caspase activation in all three types of MEFs.
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Cell Line:MEF
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Concentration:0 nM, 1.6 nM, 8 nM, 40 nM, 200 nM, 10000 nM
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Incubation Time:4 h
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Result:Suppressed STS-induced caspase activation in a dose-dependent manner.
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Cell Line:Neuro2a
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Concentration:0 nM, 40 nM, 200 nM, 10000 nM
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Incubation Time:24 h
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Result:Suppressed Etoposide-induced caspase activation in a dose-dependent manner.
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Cell Line:ARPE19
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Concentration:500 nM
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Incubation Time:24 h
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Result:Significantly inhibited Obatoclax-induced apoptosis in ARPE19 cells comparing to control.
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Cell Line:iBax cells
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Concentration:500 nM
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Incubation Time:48 h
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Result:Significantly suppressed the amount of immunoprecipitated Bax without a significant change in the total Bax expression.
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Cell Line:iBax cells
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Concentration:500 nM
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Incubation Time:48 h
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Result:Showed the frequency of the punctuated staining was significantly reduced.
In Vivo
M109S (1 mg/kg, i.p., i.v., 5 mg/kg, o.p. 10 mg/kg 1 time) is an orally bioactive cell death inhibitor penetrating blood-brain/retina-barrier[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Abca4-/-Rdh8-/- mice
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Dosage:10 mg/kg
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Administration:Oral Gavage (p.o.)
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Result:Comparing to mice with M109S, the number of AF spots was similar to that detected in the dark-adapted mice.
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Animal Model:Mice and Rat
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Dosage:Intraperitoneal injection (i.p., 1 mg/kg), Intravenous injection (i.v., 5 mg/kg), or Oral gavage (p.o., 10 mg/kg)
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Administration:Intraperitoneal injection (i.p.), Intravenous injection (i.v.), or Oral gavage (p.o.).
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Result:Showed plasma concentration reached 1.0 mg/mL (2.6 mM) within 30 min from p.o. in mice, and it remained at 596± 134 ng/mL (1.6±0.36 mM) after 24 h, the same as in rat. Plasmic M109S was 565.3±188.3 nM in rats, and 171.0±52.0 nM in retina, 222.7±74.7 nM in brain, respectively.
Chemical Information
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CAS No. 2578300-07-7
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Appearance Solid
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Masse moléculaire 375.42
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Formule C21H21N5O2
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Color White to off-white
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SMILES
CC1=NC(OC(C)=C2)=C2C(N[C@@H](C)C3=CC=C(C4=NC(C5CC5)=NO4)C=C3)=N1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (266.37 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)
In Vivo:
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 (6.66 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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 (6.66 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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.
In Vivo Dissolution Calculator
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.
Protocole
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Mammalian live/dead viability and cytotoxicity staining
Live/dead viability and cytotoxicity staining assays are based on the simultaneous detection of intracellular esterase activity in metabolically active (viable) cells and membrane integrity loss in non-viable cells. In commonly used dual-staining approaches, membrane-permeant fluorogenic substrates are converted by intracellular esterases into fluorescent products in live cells, while impermeant DNA-binding dyes selectively enter cells with compromised plasma membranes and label nucleic acids in dead or dying cells, enabling discrimination between viable and non-viable populations by fluorescence microscopy or flow cytometry.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Transepithelial/transendothelial electrical resistance assay
TEER measures electrical resistance across epithelial or endothelial monolayers cultured on permeable supports, and the readout reflects ionic conductance through the cell barrier, especially the paracellular pathway regulated by junctional integrity. TEER can be measured without destroying the monolayer and is commonly used before or during transport, permeability, barrier-disruption, and barrier-maturation experiments. TEER values are influenced by biological maturation and technical conditions; reported factors include temperature, medium formulation, passage number, electrode geometry, membrane properties, and junctional length during early monolayer maturation. Therefore, TEER should be interpreted with blank-insert subtraction, area normalization, repeated readings, and, when possible, orthogonal barrier readouts such as FITC-dextran flux or tight-junction staining.
Pureté et documentation
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Fiche technique (278 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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Instruction de manipulation (2659 KB)
Références
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 | 2.6637 mL | 13.3184 mL | 26.6368 mL | 66.5921 mL |
| 5 mM | 0.5327 mL | 2.6637 mL | 5.3274 mL | 13.3184 mL | |
| 10 mM | 0.2664 mL | 1.3318 mL | 2.6637 mL | 6.6592 mL | |
| 15 mM | 0.1776 mL | 0.8879 mL | 1.7758 mL | 4.4395 mL | |
| 20 mM | 0.1332 mL | 0.6659 mL | 1.3318 mL | 3.3296 mL | |
| 25 mM | 0.1065 mL | 0.5327 mL | 1.0655 mL | 2.6637 mL | |
| 30 mM | 0.0888 mL | 0.4439 mL | 0.8879 mL | 2.2197 mL | |
| 40 mM | 0.0666 mL | 0.3330 mL | 0.6659 mL | 1.6648 mL | |
| 50 mM | 0.0533 mL | 0.2664 mL | 0.5327 mL | 1.3318 mL | |
| 60 mM | 0.0444 mL | 0.2220 mL | 0.4439 mL | 1.1099 mL | |
| 80 mM | 0.0333 mL | 0.1665 mL | 0.3330 mL | 0.8324 mL | |
| 100 mM | 0.0266 mL | 0.1332 mL | 0.2664 mL | 0.6659 mL |
M190S Related Classifications
HY-156168 Related Classifications
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