2. Epigenetics
  3. Histone Methyltransferase
  4. EM127

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.

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EM127 Chemical Structure

EM127 Chemical Structure

CAS No. : 1886879-71-5

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Based on 1 publication(s) in Google Scholar

EM127 Related Antibodies

Top Publications Citing Use of Products

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 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].

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

EM127 Related Antibodies

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.
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2076 mL 16.0380 mL 32.0760 mL
5 mM 0.6415 mL 3.2076 mL 6.4152 mL
View the 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.

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Purity & Documentation
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
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EM127 Related Classifications

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.

Keywords:

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

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