[CAS NO. 1197824-15-9]  EN4

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PRODUCTS SPECIFICATIONS [1197824-15-9]

Catalog
HY-134761
Brand
MCE
CAS
1197824-15-9

DESCRIPTION [1197824-15-9]

Overview

MDL-
Molecular Weight416.47
Molecular FormulaC25H24N2O4
SMILESO=C(NC1=CC=CC=C1OC2=CC=C(OCC)C=C2)C3=CC=C(CNC(C=C)=O)C=C3

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

Summary

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.

Appearance

Solid


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 : 125 mg/mL ( 300.14 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 available by MCE.