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EM127

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Catalog No. T60777Cas No. 1886879-71-5

EM127 is a highly selective and potent covalent inhibitor of SMYD3 with a KD value of 13 μM.EM127 inhibits ERK1/2 phosphorylation and inhibits transcriptional regulation of SMYD3 target genes.EM127 slowly reduces methyltransferase activity over a long period of time.EM127 has potential anticancer activity and can be used to study SMYD3 positive tumors. EM127 has potential anticancer activity and can be used to study SMYD3 positive tumors.

EM127

EM127

🥰Excellent
Purity: 97.61%
Catalog No. T60777Cas No. 1886879-71-5
EM127 is a highly selective and potent covalent inhibitor of SMYD3 with a KD value of 13 μM.EM127 inhibits ERK1/2 phosphorylation and inhibits transcriptional regulation of SMYD3 target genes.EM127 slowly reduces methyltransferase activity over a long period of time.EM127 has potential anticancer activity and can be used to study SMYD3 positive tumors. EM127 has potential anticancer activity and can be used to study SMYD3 positive tumors.
Pack SizePriceAvailabilityQuantity
5 mg$105In Stock
10 mg$172In Stock
25 mg$372In Stock
50 mg$597In Stock
100 mg$955In Stock
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Purity:97.61%
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Product Introduction

Bioactivity
Description
EM127 is a highly selective and potent covalent inhibitor of SMYD3 with a KD value of 13 μM.EM127 inhibits ERK1/2 phosphorylation and inhibits transcriptional regulation of SMYD3 target genes.EM127 slowly reduces methyltransferase activity over a long period of time.EM127 has potential anticancer activity and can be used to study SMYD3 positive tumors. EM127 has potential anticancer activity and can be used to study SMYD3 positive tumors.
In vitro
In MDA-MB-231 and HCT116 cells, EM127 exhibits good anti-proliferative activity when treated with 5 μM for 24, 48, and 72 hours[1]. Additionally, at the same concentration and time points, EM127 diminishes the expression of SMYD3 target genes. However, this effect is not observed when SMYD3 is knocked out or expressed at low levels in MDA-MB-231 cells[1]. Furthermore, in both HCT116 and MDA-MB-231 cells, EM127, at concentrations of 1, 3.5, and 5 μM for 48 and 72 hours, decreases ERK1/2 phosphorylation in a dose- and time-dependent manner[1].
Chemical Properties
Molecular Weight311.76
FormulaC14H18ClN3O3
Cas No.1886879-71-5
SmilesClCC(=O)N1CCC(CC1)NC(=O)c1cc(on1)C1CC1
Storage & Solubility Information
StorageShipping with blue ice.
Solubility Information
DMSO: 20 mg/mL (64.15 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM3.2076 mL16.0380 mL32.0760 mL160.3798 mL
5 mM0.6415 mL3.2076 mL6.4152 mL32.0760 mL
10 mM0.3208 mL1.6038 mL3.2076 mL16.0380 mL
20 mM0.1604 mL0.8019 mL1.6038 mL8.0190 mL
50 mM0.0642 mL0.3208 mL0.6415 mL3.2076 mL

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