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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
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Purity: 97.55%
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 Size | Price | USA Warehouse | Global Warehouse | 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 |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:97.55%
Appearance:Solid
Color:Yellow
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| 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 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 20 mg/mL (64.15 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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