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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $32 | In Stock | |
5 mg | $72 | In Stock | |
10 mg | $89 | In Stock | |
25 mg | $197 | In Stock | |
50 mg | $297 | In Stock | |
100 mg | $447 | In Stock | |
1 mL x 10 mM (in DMSO) | $79 | 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. |
Alias | EN4 MYC inhibitor |
Molecular Weight | 416.47 |
Formula | C25H24N2O4 |
Cas No. | 1197824-15-9 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 250 mg/mL (600.28 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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