EN4

Catalog No.S9807

For research use only.

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

CAS No. 1197824-15-9

Purity & Quality Control

Choose Selective Myc Inhibitors

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

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]

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]

Protocol (from reference)

Cell Research:

[1]

  • 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.

Animal Research:

[1]

  • Animal Models: C.B17 SCID female mice (6-8 weeks old)
  • Dosages: 50 mg/kg
  • Administration: IP

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 416.47
Formula

C25H24N2O4

CAS No. 1197824-15-9
Storage 3 years -20°C powder
2 years -80°C in solvent

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

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04820361 Not yet recruiting Drug: Cannabis sativa L. folium cum flore|Drug: Placebo Pain Neuropathic Albina Nowak MD|Swiss National Science Foundation|University of Zurich June 15 2022 Not Applicable

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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