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EN4

Catalog No. T9061 CAS 1197824-15-9

Synonyms: EN4 MYC inhibitor

EN4 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.

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EN4, CAS 1197824-15-9

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Purity: 98%

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Description

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.

Synonyms	EN4 MYC inhibitor
Molecular Weight	416.477
Formula	C25H24N2O4
CAS No.	1197824-15-9

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 250 mg/mL (600.28 mM), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Lydia Boike, et al. Discovery of a Functional Covalent Ligand Targeting an Intrinsically Disordered Cysteine within MYC. Cell Chem Biol. 2021 Jan 21;28(1):4-13.e17.

Related compound libraries

This product is contained In the following compound libraries：

Cell Cycle Compound Library Covalent Inhibitor Library Bioactive Compound Library

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Related compounds with same targets

Moracin T Moracin D Coronarin D Sanggenol L Aaptamine 10074-A4 10074-G5 sAJM589

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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.

Keywords

EN4 1197824-15-9 细胞周期 c-Myc ligand Myc tumorigenesis transcriptional inhibit EN4 MYC inhibitor Inhibitor EN 4 covalent C171 EN-4 inhibitor

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