2. Epigenetics
  3. Histone Methyltransferase
  4. EM127

EM127 

Cat. No.: HY-151379
Handling Instructions

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.

EM127 Chemical Structure

EM127 Chemical Structure

CAS No. : 1886879-71-5

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EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT8

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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].

IC50 & Target[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

311.76

Formula

C14H18ClN3O3
CAS No.
SMILES

O=C(C1=NOC(C2CC2)=C1)NC3CCN(C(CCl)=O)CC3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

EM1271886879-71-5EM 127EM-127Histone MethyltransferaseSMYD3 positive tumourscancerMDA-MB-231HCT116Cys186ERK1/2Inhibitorinhibitorinhibit

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