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EN4 (EN4 MYC inhibitor) MYC inhibitor is a covalent ligand that targets cysteine 171 (C171) of MYC. It is selective for c-MYC over N-MYC and L-MYC, and inhibits MYC transcriptional activity, downregulates MYC targets, and impairs tumorigenesis.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $32 | In Stock | In Stock | |
| 5 mg | $72 | In Stock | In Stock | |
| 10 mg | $89 | In Stock | In Stock | |
| 25 mg | $197 | In Stock | In Stock | |
| 50 mg | $297 | In Stock | In Stock | |
| 100 mg | $447 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $79 | In Stock | In Stock |
| Description | EN4 (EN4 MYC inhibitor) MYC inhibitor is a covalent ligand that targets cysteine 171 (C171) of MYC. It is selective for c-MYC over N-MYC and L-MYC, and inhibits MYC transcriptional activity, downregulates MYC targets, and impairs tumorigenesis. |
| In vitro | EN4 (50 μM;?for 60 hours) treatment significantly decreases the protein levels of representative MYC-regulated target genes, including CDK2 and CDC25A.?EN4 treatment also substantially reduces MYC levels.EN4 shows the strongest inhibition of both MYC/MAX binding to its DNA consensus sequence in vitro as well as MYC transcriptional activity in cells.?EN4 inhibited MYC/MAX binding to the E-box response element DNA consensus sequence in a dose-responsive manner with an IC50 value of 6.7 μM.?EN4 also inhibits MYC luciferase reporter activity in a dose-responsive manner with an IC50 value of 2.8 μM.EN4 (1-50 μM; for 72 hours) treatment significantly impaires 231MFP breast cancer cell proliferation in a dosedependent manner, with >90% inhibition of proliferation at 50 μM.EN4 (50 μM;?for 2 hours) treatment significantly reduced MYC thermal stability in 231MFP breast cancer cells. |
| Molecular Weight | 416.47 |
| Formula | C25H24N2O4 |
| Cas No. | 1197824-15-9 |
| Smiles | CCOc1ccc(Oc2ccccc2NC(=O)c2ccc(CNC(=O)C=C)cc2)cc1 |
| Relative Density. | 1.202 g/cm3 (Predicted) |
| 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: 245 mg/mL (588.28 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+90% Corn Oil: 3.3 mg/mL (7.92 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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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.
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.
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