PF-9363

PF-9363 is an inhibitor of lysine acetyltransferase 6A (KAT6A), also known as monocytic leukemia zinc finger protein (MOZ) and KAT6B, also known as MOZ-related factor (MORF; K_is = 0.27 and 2.4 nM, respectively).¹ It is selective for KAT6A and KAT6B over KAT7, KAT5, and KAT8 (K_is = 70, 420, and 670 nM, respectively). PF-9363 reduces the proliferation of, and the levels of acetylation of histone 3 lysine 23 (H3K23Ac) and lysine 14 (H3K14Ac) in, ZR-75-1 breast epithelial carcinoma cells (IC₅₀s = 0.37, 0.85, and 120 nM, respectively). It reduces tumor levels of H3K23Ac and tumor volume without affecting body weight in a ZR-75-1 breast cancer mouse xenograft model when administered at doses of 0.03, 03, or 5 mg/kg per day. PF-9363 (1 mg/kg per day) reduces tumor volume and increases survival in a patient-derived xenograft (PDX) mouse model of breast cancer.

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1. Sharma, S., Chung, C.-Y., Uryu, S., et al. Discovery of a highly potent, selective, orally bioavailable inhibitor of KAT6A/B histone acetyltransferases with efficacy against KAT6A-high ER+ breast cancer. Cell Chem. Biol. 30, (2023).