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EN4

Catalog No. T9061 CAS 1197824-15-9

Synonyms: EN4 MYC inhibitor

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.

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EN4, CAS 1197824-15-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 32.00
5 mg	In stock	$ 72.00
10 mg	In stock	$ 89.00
25 mg	In stock	$ 197.00
50 mg	In stock	$ 297.00
100 mg	In stock	$ 447.00
1 mL * 10 mM (in DMSO)	In stock	$ 79.00

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Purity: 98.19%

Biological Description

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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	416.47
Formula	C25H24N2O4
CAS No.	1197824-15-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 250 mg/mL (600.28 mM), Sonification is recommended.

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：

Inhibitor Library Anti-Cancer Active Compound Library Bioactive Compounds Library Max Apoptosis Compound Library Anti-Cancer Metabolism Compound Library Wnt/Hedgehog/Notch Compound Library Covalent Inhibitor Library Bioactive Compound Library Anti-Cancer Compound Library Glycolysis Compound Library

Related Products

Related compounds with same targets

10074-G5 MYCi361 KSI-3716 m-Se3 Mycro 3 Coronarin D Aaptamine ML327

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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 Cell Cycle/Checkpoint c-Myc ligand Myc EN-4 tumorigenesis transcriptional inhibit EN 4 Inhibitor EN4 MYC inhibitor covalent C171 inhibitor

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