NU 9056

NU 9056 was originally identified as an inhibitor of TIP60, also known as lysine acetyltransferase 5 (KAT5; IC₅₀ = 2 µM).¹ However, it has been shown that NU 9056 is thiol-reactive in a cell-free assay and inhibits multiple targets in biochemical and cell-based assays, indicating it is a non-selective interference compound.² NU 9056 inhibits the growth of LNCaP, CWR22Rυ1, and PC3 prostate cancer cells (GI₅₀s = 24, 7.5, and 27 µM, respectively) and induces apoptosis in LNCaP cells.¹ It inhibits activation of the NOD-like receptor protein 3 (NLRP3) inflammasome in LPS-primed nigericin-induced primary mouse peritoneal macrophages.³ NU 9056 (10 mg/kg) decreases lung injury in a mouse model of LPS-induced endotoxemia. It increases freezing time seven days after fear conditioning, indicating enhanced remote memory, in mice when administered at a dose of 2 µg/g.⁴

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1. Coffey, K., Blackburn, T.J., Cook, S., et al. Characterisation of a Tip60 specific inhibitor, NU9056, in prostate cancer. PLoS One 7(10), e45539 (2012).

2. Dahlin, J.L., Nelson, K.M., Strasser, J.M., et al. Assay interference and off-target liabilities of reported histone acetyltransferase inhibitors. Nat. Commun. 8(1), 1527 (2017).

3. Zhang, Y., Luo, L., Xu, X., et al. Acetylation is required for full activation of the NLRP3 inflammasome. Nat. Commun. 14(1), 8396 (2023).

4. Narkaj, K., Stefanelli, G., Wahdan, M., et al. Blocking H2A.Z incorporation via Tip60 inhibition promotes systems consolidation of fear memory in mice. eNeuro 5(5), (2018).