EN4 MYC inhibitor

EN4 is a functional Covalent Ligand Targeting an Intrinsically Disordered Cysteine within MYC. EN4 functionally and covalently targets an intrinsically disordered region in MYC. EN4 directly targets MYC in cells and reduces MYC and MAX thermal stability. EN4 inhibits MYC activity, downregulates MYC targets, and impairs tumorigenesis. MYC is a major oncogenic transcriptional driver of most human cancers that has remained intractable to direct targeting because much of MYC is intrinsically disordered.

Product information

CAS Number: 1197824-15-9

Molecular Weight: 416.47

Formula: C25H24N2O4

Chemical Name: 4-(acrylamidomethyl)-N-(2-(4-ethoxyphenoxy)phenyl)benzamide

Smiles: CCOC1=CC=C(C=C1)OC1=CC=CC=C1NC(=O)C1=CC=C(CNC(=O)C=C)C=C1

InChiKey: DKOWGKKELPCHEG-UHFFFAOYSA-N

InChi: InChI=1S/C25H24N2O4/c1-3-24(28)26-17-18-9-11-19(12-10-18)25(29)27-22-7-5-6-8-23(22)31-21-15-13-20(14-16-21)30-4-2/h3,5-16H,1,4,17H2,2H3,(H,26,28)(H,27,29)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO: 83 mg/mL(199.29 mM).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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.

In Vivo:

EN4 treatment initiated after establishment of a 231MFP breast tumor xenograft in immune-deficient mice also significantly attenuates tumor growth in vivo.

References:

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

Products are for research use only. Not for human use.