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EN4

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Catalog No. T9061Cas No. 1197824-15-9

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.

EN4

EN4

🥰Excellent
Purity: 98.51%
Catalog No. T9061Cas No. 1197824-15-9
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 SizePriceAvailabilityQuantity
1 mg$32In Stock
5 mg$72In Stock
10 mg$89In Stock
25 mg$197In Stock
50 mg$297In Stock
100 mg$447In Stock
1 mL x 10 mM (in DMSO)$79In Stock
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Purity:98.51%
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Product Introduction

Bioactivity
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.
Chemical Properties
Molecular Weight416.47
FormulaC25H24N2O4
Cas No.1197824-15-9
SmilesCCOc1ccc(Oc2ccccc2NC(=O)c2ccc(CNC(=O)C=C)cc2)cc1
Relative Density.1.202 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM2.4011 mL12.0057 mL24.0113 mL120.0567 mL
5 mM0.4802 mL2.4011 mL4.8023 mL24.0113 mL
10 mM0.2401 mL1.2006 mL2.4011 mL12.0057 mL
20 mM0.1201 mL0.6003 mL1.2006 mL6.0028 mL
50 mM0.0480 mL0.2401 mL0.4802 mL2.4011 mL
100 mM0.0240 mL0.1201 mL0.2401 mL1.2006 mL

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