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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 Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $105 | In Stock | |
10 mg | $172 | In Stock | |
25 mg | $372 | In Stock | |
50 mg | $597 | In Stock | |
100 mg | $955 | In Stock |
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]. |
Molecular Weight | 311.76 |
Formula | C14H18ClN3O3 |
Cas No. | 1886879-71-5 |
Smiles | ClCC(=O)N1CCC(CC1)NC(=O)c1cc(on1)C1CC1 |
Storage | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 20 mg/mL (64.15 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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