JG-2016

JG-2016 is an inhibitor of histone acetyltransferase 1 (HAT1; IC₅₀ = 14.8 µM).¹ It is selective for HAT1 over lysine acetyltransferase 2A (KAT2A/GCN5) and p300/CBP-associated factor (PCAF), for which it has no activity, KAT5, KAT6B, and KAT7 (IC₅₀s = >100, >100, and 84.82 µM, respectively), CREB-binding protein (CBP), and p300 (IC₅₀s = 90.41 and 74.25 µM, respectively). JG-2016 (20 µM) reduces acetylation of histone H4 lysine 5 (H4K5) and H4K12 in hTert-HME1 mammary epithelial cells. It reduces the growth of HCC1806 triple-negative breast cancer and A549 lung cancer cells (EC₅₀s = 10.4 and 1.9 µM, respectively). JG-2016 reduces intratumoral H4K12 acetylation in an A549 mouse xenograft model in a dose-dependent manner. It also reduces tumor growth in an A549 mouse xenograft model when administered at doses of 50 and 100 mg/kg once every three days.

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1. Gaddameedi, J.D., Chou, T., Geller, B.S., et al. An acetyl-click screening platform identifies small-molecule inhibitors of histone acetyltransferase 1 (HAT1). J. Med. Chem. 66(8), 5774-5801 (2023).