1. Apoptosis
  2. c-Myc
  3. EN4

EN4 

Cat. No.: HY-134761 Purity: 96.05%
Handling Instructions

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

For research use only. We do not sell to patients.

EN4 Chemical Structure

EN4 Chemical Structure

CAS No. : 1197824-15-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 275 In-stock
Estimated Time of Arrival: December 31
5 mg USD 250 In-stock
Estimated Time of Arrival: December 31
10 mg USD 450 In-stock
Estimated Time of Arrival: December 31
25 mg USD 850 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1350 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1950 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

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

In Vitro

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[1].
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[1].
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[1].
EN4 (50 μM; for 2 hours) treatment significantly reduced MYC thermal stability in 231MFP breast cancer cells[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: 231MFP breast cancer cells
Concentration: 1 μM, 10 μM, 50 μM
Incubation Time: 72 hours
Result: Significantly impaired 231MFP breast cancer cell proliferation in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: 231MFP breast cancer cells
Concentration: 50 μM
Incubation Time: 60 hours
Result: The protein levels of CDK2 and CDC25A were significantly lowered.
In Vivo

EN4 (50 mg/kg; intraperitoneal injection; daily; for 3 weeks) treatment significantly attenuated tumor growth in 231MFP breast tumor xenograft mice[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: SCID mice injected with 231MFP breast cancer cells[1]
Dosage: 50 mg/kg
Administration: Intraperitoneal injection; daily; for 3 weeks
Result: Significantly attenuated tumor growth in vivo.
Molecular Weight

416.47

Formula

C₂₅H₂₄N₂O₄

CAS No.
SMILES

O=C(NC1=CC=CC=C1OC2=CC=C(OCC)C=C2)C3=CC=C(CNC(C=C)=O)C=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

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

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4011 mL 12.0057 mL 24.0113 mL
5 mM 0.4802 mL 2.4011 mL 4.8023 mL
10 mM 0.2401 mL 1.2006 mL 2.4011 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.08 mg/mL (4.99 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (4.99 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.99 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

EN4EN 4EN-4c-MycMycC171covalentligandtranscriptionaltumorigenesisInhibitorinhibitorinhibit

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