M443
Based on 3 publication(s) in Google Scholar
M443 is an irreversible and specific inhibitor of MRK, with an IC50<125 nM.
For research use only. We do not sell to patients.
- Purity : 99.92%
- CAS No.: 1820684-31-8
- Formula: C31H30F3N7O2
- Molecular Weight:589.61
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) M443
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Biological Activity
Description
IC50 & Target
IC50: <125 nM (MRK)[1].
In Vitro
MRK depletion decreases cell viability after IR by 33% of control at 3 Gy. Similarly, the clonogenic assay shows a significant decrease in survival with a dose enhancement factor (DEF) of 1.6 at 10% viability. MRK activation by IR is maximal at 30 minutes after exposure to radiation. Therefore, for subsequent analysis, this time point is used. In both cell cultures, the IR-stimulated activation of MRK, Chk2, and p38 is greatly inhibited by 500 nM M443. Cells are seeded on coverslips, pretreated with 500 nM M443 or vehicle, exposed to 6 Gy of IR, fixed at different times after IR and processed for immunofluorescence with the MPM2 phospho-specific antibody that specifically stains mitotic cells. In contrast to control cells, the M443-treated cells fail to arrest after IR and maintained a similar mitotic index as the nonirradiated cells. Thus, inhibition of MRK leads to inhibition of Chk2 and failure to arrest in the cell cycle in response to IR-induced DNA damage[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1820684-31-8
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Appearance Solid
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Molecular Weight 589.61
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Formula C31H30F3N7O2
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Color Light yellow to yellow
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SMILES
FC(F)(F)C1=CC(NC(C2=CC(NC3=NC=CC(C4CN(C(C=C)=O)CCC4)=N3)=C(C)C=C2)=O)=CC(N5C=NC(C)=C5)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Cell Res
SMYD5 is a ribosomal methyltransferase that catalyzes RPL40 lysine methylation to enhance translation output and promote hepatocellular carcinoma. [Abstract]2024 Sep;34(9):648-660. PMID: 39103523 -
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Solvent & Solubility
In Vitro:
DMSO : 55 mg/mL (93.28 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocols
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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.
Purity & Documentation
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Data Sheet (279 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6960 mL | 8.4802 mL | 16.9604 mL | 42.4009 mL |
| 5 mM | 0.3392 mL | 1.6960 mL | 3.3921 mL | 8.4802 mL | |
| 10 mM | 0.1696 mL | 0.8480 mL | 1.6960 mL | 4.2401 mL | |
| 15 mM | 0.1131 mL | 0.5653 mL | 1.1307 mL | 2.8267 mL | |
| 20 mM | 0.0848 mL | 0.4240 mL | 0.8480 mL | 2.1200 mL | |
| 25 mM | 0.0678 mL | 0.3392 mL | 0.6784 mL | 1.6960 mL | |
| 30 mM | 0.0565 mL | 0.2827 mL | 0.5653 mL | 1.4134 mL | |
| 40 mM | 0.0424 mL | 0.2120 mL | 0.4240 mL | 1.0600 mL | |
| 50 mM | 0.0339 mL | 0.1696 mL | 0.3392 mL | 0.8480 mL | |
| 60 mM | 0.0283 mL | 0.1413 mL | 0.2827 mL | 0.7067 mL | |
| 80 mM | 0.0212 mL | 0.1060 mL | 0.2120 mL | 0.5300 mL |