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EN4-2 is a cell penetrant, potent and selective covalent c-MYC inhibitor that targets cysteine 171 located within a predicted intrinsically disordered region of MYC. EN4-2 inhibits MYC transcriptional activity, downregulates multiple MYC transcriptional targets, reduces MYC and MAX thermal stability, and impairs tumorigenesis.
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
Discovery of a Functional Covalent Ligand Targeting an Intrinsically Disordered Cysteine within MYC.
Lydia Boike et al.
Cell chemical biology, 28(1), 4-13 (2020-09-24)
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. Here, we have performed a cysteine-reactive covalent ligand screen to identify compounds that could disrupt
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