EZH2-IN-23 (Compound 25) is an EZH2 inhibitor, exhibiting potent enzymatic inhibition against the PRC2 complex [EZH2, EED, SUZ12, AEBP2, and RbAp48] with an IC50 of 0.8 nM. It inhibits H3K27 trimethylation in cells with an IC50 of 40 nM. In rats, EZH2-IN-23 demonstrates excellent pharmacokinetic properties, achieving 100% oral bioavailability.
Target-Kategorie:
Histone Methyltransferase
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