EM127
Based on 1 Customer Validation
EM127 (compound 11c) is a SMYD3 covalent inhibitor with high selectivity, high affinity (KD=13 μM) and site-specificity. EM127 effectively inhibits ERK1/2 phosphorylation and reduces transcriptional regulation of SMYD3 target genes. EM127 effectively and prolongedly impairs methyltransferase activity. EM127 can be used in cancer research, particularly in SMYD3 positive tumours.
For research use only. We do not sell to patients.
- Purity: 99.94%
- CAS No.: 1886879-71-5
- Formula: C14H18ClN3O3
- Molecular Weight:311.76
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Storage:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Posttranslational Modification Library
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All Histone Methyltransferase Isoforms
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Biological Activity
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SMYD3 |
EM127 (5 μM; 24, 48, 72 h) shows good anti-proliferative activity in MDA-MB-231and HCT116 cells[1].
EM127 (5 μM; 24, 48, 72 h) attenuates the expression of SMYD3 target genes while does not affect expression when SMYD3 is knocked out or expressed at low levels in MDA-MB-231 cells[1].
EM127 (1, 3.5, 5 μM; 48, 72 h) decreases ERK1/2 phosphorylation in a dose- and time-dependent manner in HCT116 and MDA-MB-231cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231, HCT116 cells
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Concentration:5 μM
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Incubation Time:24, 48, 72 h
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Result:Significantly retarded cell proliferation by 48 h.
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Cell Line:MDA-MB-231 cells
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Concentration:0.5, 3.5, 5 μM
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Incubation Time:48 h
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Result:Significantly reduced the expression of CDK2 and C-MET, the known SMYD3 regulated genes.
Attenuated the abundance of mRNAs of the extracellular matrix component fibronectin 1 (FN1) and N-cadherin (N-CAD).
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Cell Line:HCT116, MDA-MB-231cells
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Concentration:1, 3.5, 5 μM
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Incubation Time:48, 72 h
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Result:Attenuated ERK1/2 phosphorylation and induced PARP processing at the same concentrations that retarded cell proliferation.
Chemical Information
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CAS No. 1886879-71-5
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Appearance Solid
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Molecular Weight 311.76
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Formula C14H18ClN3O3
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Color White to off-white
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SMILES
O=C(C1=NOC(C2CC2)=C1)NC3CCN(C(CCl)=O)CC3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvent & Solubility
DMSO : 25 mg/mL (80.19 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 (stored under nitrogen). 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 (stored under nitrogen). 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)
Purity & Documentation
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Data Sheet (271 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 (stored under nitrogen). 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 | 3.2076 mL | 16.0380 mL | 32.0760 mL | 80.1899 mL |
| 5 mM | 0.6415 mL | 3.2076 mL | 6.4152 mL | 16.0380 mL | |
| 10 mM | 0.3208 mL | 1.6038 mL | 3.2076 mL | 8.0190 mL | |
| 15 mM | 0.2138 mL | 1.0692 mL | 2.1384 mL | 5.3460 mL | |
| 20 mM | 0.1604 mL | 0.8019 mL | 1.6038 mL | 4.0095 mL | |
| 25 mM | 0.1283 mL | 0.6415 mL | 1.2830 mL | 3.2076 mL | |
| 30 mM | 0.1069 mL | 0.5346 mL | 1.0692 mL | 2.6730 mL | |
| 40 mM | 0.0802 mL | 0.4009 mL | 0.8019 mL | 2.0047 mL | |
| 50 mM | 0.0642 mL | 0.3208 mL | 0.6415 mL | 1.6038 mL | |
| 60 mM | 0.0535 mL | 0.2673 mL | 0.5346 mL | 1.3365 mL | |
| 80 mM | 0.0401 mL | 0.2005 mL | 0.4009 mL | 1.0024 mL |
EM127 Related Classifications
HY-151379 Related Classifications
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