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Chemical Structure| 1197824-15-9 Chemical Structure| 1197824-15-9

Structure of EN4
CAS No.: 1197824-15-9

Chemical Structure| 1197824-15-9

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EN4 is a covalent ligand targeting cysteine 171 (C171) of MYC, with high selectivity and antitumor effects. It effectively downregulates MYC targets, holding important applications in cancer research.

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Product Details of EN4

CAS No. :1197824-15-9
Formula : C25H24N2O4
M.W : 416.47
SMILES Code : O=C(NC1=CC=CC=C1OC2=CC=C(OCC)C=C2)C3=CC=C(CNC(C=C)=O)C=C3
MDL No. :MFCD13582116

Safety of EN4

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Related Pathways of EN4

Hedgehog

Isoform Comparison

Biological Activity

Description
EN4 is a covalent ligand designed to target cysteine 171 (C171) of MYC. It exhibits selectivity for c-MYC over N-MYC and L-MYC. Moreover, EN4 effectively inhibits MYC transcriptional activity.

In Vitro:

Cell Line
Concentration Treated Time Description References
Trypanosoma brucei brucei (strain 427) 0.54 μM (IC50) 48 hours Evaluate the growth inhibitory activity of the compound against T. b. brucei, with an EC50 of 0.54 μM. PMC10843616
Trypanosoma brucei gambiense (130R) 0.13 μM (IC50) 68 hours Evaluate the growth inhibitory activity of the compound against T. b. gambiense, with an EC50 of 0.13 μM. PMC10843616
Trypanosoma brucei rhodesiense (STIB 900) 0.14 μM (IC50) 70 hours Evaluate the growth inhibitory activity of the compound against T. b. rhodesiense, with an EC50 of 0.14 μM. PMC10843616
Human hepatocarcinoma cells (Hep G2, CRL-11997TM) 0.01–300 μM 72 hours Evaluate the cytotoxicity of the compound against Hep G2 cells, with a CC50 >75 μM. PMC10843616
Mouse L929 fibroblasts 25, 50, 100 μg/mL 8 hours To evaluate the cytotoxicity of EN4 on eukaryotic cells. EN4 exhibited time- and concentration-dependent cytotoxicity within the range of MBCs. PMC3535986

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C.B17 SCID mice 231MFP breast tumor xenograft model Intraperitoneal injection 50 mg/kg Once daily until the end of the experiment Evaluating the anti-tumor effects of EN4 in vivo, EN4 significantly inhibited tumor growth PMC7854864

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.40mL

0.48mL

0.24mL

12.01mL

2.40mL

1.20mL

24.01mL

4.80mL

2.40mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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