2055397-18-5

MOZ-IN-3 is an inhibitor of lysine acetyltransferase 6A (KAT6A/MOZ) and KAT6B/MORF (IC₅₀s = 8 and 28 nM, respectively). It is selective for KAT6A and KAT6B over KAT5 and KAT7 (IC₅₀s = 224 and 342 nM, respectively). MOZ-IN-3 induces cell cycle arrest in and inhibits proliferation of mouse embryonic fibroblasts (IC₅₀ = 2.4 μM) and inhibits proliferation of EMRK1184 lymphoma cells (IC₅₀ = 2.3 μM). It induces genetic and morphological changes associated with cellular senescence without inducing DNA damage, apoptosis, or necrosis. MOZ-IN-3 (10 μM) decreases global levels of acetylated histone H3 lysine 14 (H3K14Ac) by 49% and reduces H3K9Ac levels at the transcription start sites of Ezh2, Melk, and E2f2.

MOZ-IN-3 is a highly potent and selective inhibitor of lysine acetyltransferases, KAT6A and KAT6B.

MOZ/MORF

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[1] JONATHAN B. BAELL. Inhibitors of histone acetyltransferases KAT6A/B induce senescence and arrest tumour growth[J]. Nature, 2018, 560 7717: 253-257. DOI: 10.1038/s41586-018-0387-5