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EPZ-6438

    Detailed Description

    EPZ-6438EPZ-6438 is a potent, selective, and orally bioavailable small-molecule inhibitor of EZH2 enzymatic activity with Ki value of 2.5±0.5 nM.

    IC50 Value: 2.5±0.5 nM (PRC2-containing wild-type EZH2) [1]

    Target: EZH2; HMTase

    in vitro: EPZ-6438 inhibited the activity of human PRC2-containing wild-type EZH2 with an inhibition constant (Ki) value of 2.5 ± 0.5 nM, and similar potency was observed for EZH2 proteins bearing all known lymphoma change-of-function mutations.

    Target:Others

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