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1093/infdis/jiw129
Molecular modeling studies of the novel inhibitors of DNA methyltransferases SGI-1027 and CBC12: implications for the mechanism of inhibition of DNMTs
It is a weak inhibitor of PKA with an IC50 of 30 μM
CFTR channel pharmacology: insight from a flock of clones
EN4 MYC inhibitor - CAS# 1197824-15-9 degrader-1 1093/infdis/jiw129EN4 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
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