Chemical Name: 2-Fluoro-N'-(3-fluoro-5-(pyridin-2-yl)benzoyl)benzenesulfonohydrazide
Biological ActivityHigh affinity and competitive lysine acetyltransferase 6A (KAT6A/MOZ) inhibitor (Kd = 2 nM). Displays >250-fold affinity for KAT6A compared to KAT5 and KAT7. Induces cell-cycle exit and cellular senescence, and inhibits growth of B-cell lymphoma cells in vitro (IC50 = 0.25 μM). Reduces H3K9ac in tumor cells, and decreases tumor burden and spleen weight in a mouse lymphoma model.
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Inhibitors of histone acetyltransferases KAT6A/B induce senescence and arrest tumour growth.
Baell et al.
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