1886879-71-5
1886879-71-5 structure
- Name: EM127
- Chemical Name: EM127
- CAS Number: 1886879-71-5
- Molecular Formula: C14H18ClN3O3
- Molecular Weight: 311.76
- Catalog: Signaling Pathways Epigenetics Histone Methyltransferase
- Create Date: 2022-10-15 11:46:27
- Modify Date: 2024-04-02 20:03:08
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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[1].
| Name | EM127 |
|---|
| Description | 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[1]. |
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| Related Catalog | |
| Target |
SMYD3 |
| In Vitro | 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]. Cell Proliferation Assay[1] Cell Line: MDA-MB-231, HCT116 cells Concentration: 5 μM Incubation Time: 24, 48, 72 h Result: Significantly retarded cell proliferation by 48 h. RT-PCR[1] Cell Line: MDA-MB-231 cells Concentration: 0.5, 3.5, 5 μM Incubation Time: 48 h 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). Western Blot Analysis[1] Cell Line: HCT116, MDA-MB-231cells Concentration: 1, 3.5, 5 μM Incubation Time: 48, 72 h Result: Attenuated ERK1/2 phosphorylation and induced PARP processing at the same concentrations that retarded cell proliferation. |
| References |
| Molecular Formula | C14H18ClN3O3 |
|---|---|
| Molecular Weight | 311.76 |