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NU9056 is a potent and selective KAT5 (Tip60) histone acetyltransferase inhibitor (IC₅₀ are < 2 μM, 60 μM, 36 μM, and >100 μM for KAT5, p300, pCAF and GCN5, respectively), identified by a high-throughput screening. NU9056 inhibited cellular proliferation in a panel of prostate cancer cell lines (50% growth inhibition, 8-27 μM) and induced apoptosis via activation of caspase 3 and caspase 9 in a concentration- and time-dependent manner. The protein levels of androgen receptor, prostate specific antigen, p53 and p21 were decreased in response to treatment with NU9056. Furthermore, pre-treatment with NU9056 inhibited both ATM phosphorylation and Tip60 stabilization in response to ionizing radiation. NU9056 is a very useful chemical probe to study Tip60 (KAT5) histone acetyltransferase function.?

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How to Use:

• In vitro:? NU9056 was used at 24 μM final concentration in vitro and in cellular assays.
• In vivo: ?n/a

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Reference:

1. 1. Coffey K, et al. Characterisation of a Tip60 specific inhibitor, NU9056, in prostate cancer. (2012) PLoS One. 7(10):e45539.?

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