Home Cell Cycle Myc inhibitor EN4 For research use only.

EN4

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

EN4 Chemical Structure

EN4 Chemical Structure

CAS: 1197824-15-9

Selleck's EN4 has been cited by 1 publication

Purity & Quality Control

Batch: S980701 DMSO] 83 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 98.82%
98.82

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Biological Activity

Description EN4, a covalent ligand that targets cysteine 171 (C171) of MYC, is selective for c-MYC over N-MYC and L-MYC. EN4 inhibits MYC transcriptional activity, downregulates MYC targets, and impairs tumorigenesis.
Targets
MYC [1]
In vitro
In vitro

EN4 directly targets MYC in cells, reduces MYC and MAX thermal stability, inhibits MYC transcriptional activity, downregulates multiple MYC transcriptional targets, and impairs tumorigenesis. EN4 treatment significantly impairs 231MFP breast cancer cell proliferation in a dose- and time-dependent manner. EN4 impairs the cell survival of MYC transformed mammary epithelial MCF10A cells, but not parental MCF10A cells that are not dependent on MYC.[1]
Cell Research Cell lines 231MFP, MDA-MB-231, HEK293T and MCF10A cells
Concentrations 50 μM
Incubation Time 24 h
Method

231MFP cells are seeded into 6 cm dishes and cells are treated with DMSO vehicle or EN4 (50 μM) for 24 h. Cells are harvested by scraping and RNA is isolated using Qiagen RNeasy mini kit with Qiagen DNase max kit to remove any DNA contamination. mRNA is enriched for using Oligo dT beads from the KAPA mRNA Capture Kit.
In Vivo
In vivo

EN4 treatment initiated after establishment of a 231MFP breast tumor xenograft in immune-deficient mice also significantly attenuates tumor growth in vivo.[1]
Animal Research Animal Models C.B17 SCID female mice (6-8 weeks old)
Dosages 50 mg/kg
Administration IP
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04820361 Recruiting
Pain Neuropathic
Albina Nowak MD|Swiss National Science Foundation|University of Zurich
 July 7 2022 Not Applicable
NCT05521737 Recruiting
Electroacupuncture|Acupuncture|Diabetic Polyneuropathy|Diabetic Peripheral Neuropathy|Diabetic Peripheral Neuropathic Pain|Nerve Conduction
Instituto Mexicano del Seguro Social|National Polytechnic Institute Mexico|Instituto Nacional de Salud Publica Mexico|Escuela Superior de Medicina Instituto Politécnico Nacional|Escuela Nacional de Medicina y Homeopatía Instituto Politécnico Nacional|Universidad Nacional Autonoma de Mexico|Facultad de Estudios Superiores Iztacala Universidad Nacional Autónoma de Mexico|Facultad de Estudios Superiores Zaragoza Universidad Nacional Autónoma de Mexico|Facultad de Medicina UNAM
 November 1 2021 Not Applicable

Chemical Information & Solubility

Molecular Weight 416.47 Formula

C25H24N2O4
CAS No. 1197824-15-9 SDF --
Smiles CCOC1=CC=C(OC2=C(NC(=O)C3=CC=C(CNC(=O)C=C)C=C3)C=CC=C2)C=C1
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 83 mg/mL ( (199.29 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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In vivo Formulation Calculator

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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