NU 9056 是一种有效且选择性的 KAT5 组蛋白乙酰转移酶抑制剂，IC50 为 2 μM。 NU 9056 阻断 DNA 损伤反应并抑制前列腺癌细胞系中的蛋白质乙酰化。

NU 9056 is an effective and selective inhibitor of KAT5 histone acetyltransferase with an IC50 of 2 μM. NU 9056 blocks DNA damage response and inhibits protein acetylation in prostate cancer cell lines.

NU 9056 shows IC50s of 60, 36, and >100 μM for KAT5, p300, pCAF and GCN5, respectively. In LNCaP cells, NU 9056 (17 μM, 24 μM, 36 μM) activates both caspase 3 and caspase 9 in a time- and concentration-dependent manner thereby inducing apoptosis. NU 9056 (2.5 μM, 5 μM, 10 μM, 20 μM, 40 μM) decreases the levels of acetylated histone H4K16, H3K14 and H4K8. NU 9056 causes a reduction of androgen receptor, prostate specific antigen, p53 and p21 protein levels[2].

In mice, NU 9056 (2 μg/g) inhibits Tip60 and reduces H2A.Z binding at the the +1 nucleosome of Arc and Syp and the -1 nucleosome of Arc. NU 9056 increases the acetylation at the +1 nucleosome of Gria4 and the -1 nucleosome of Fos, Tacstd2, and Gria4[1].

1450644-28-6

C6H4N2S4

232.37

DMSO:<10mg>Powder: -20°C for 3 years
In solvent: -80°C for 2 years