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MYC inhibitor EN4

Chemical Structure : MYC inhibitor EN4

CAS No.: 1197824-15-9

MYC inhibitor EN4

Catalog No.: PC-73141Not For Human Use, Lab Use Only.

MYC inhibitor EN4 is a covalent ligand and inhibitor of MYC, targets cysteine 171 of MYC and inhibits MYC transcriptional activity (EC50=2.8 uM).

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Biological Activity

MYC inhibitor EN4 is a covalent ligand and inhibitor of MYC, targets cysteine 171 of MYC and inhibits MYC transcriptional activity (EC50=2.8 uM).
EN4 inhibited MYC/MAX binding to the E-box response element DNA consensus sequence in a dose-responsive manner with EC50 of 6.7 uM.
EN4 directly and covalently modifies pure full-length c-MYC protein at C171 to inhibit MYC/MAX DNA binding in vitro.
EN4 engages MYC in cells, reduced MYC and MAX thermal stability in 231MFP breast cancer cells.
EN4 downregulates multiple MYC transcriptional targets, and impairs tumorigenesis.

Physicochemical Properties

M.Wt 416.477
Formula C25H24N2O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Month
Shipping
Solubility

Chemical Name/SMILES

References

1. Lydia Boike, et al. Cell Chem Biol. 2021 Jan 21;28(1):4-13.e17.

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