NU9056 is a potent and selective Tip60 (KAT5) histone acetyltransferase inhibitor with an of 2 μM. NU9056 shows >16-fold selectivity for Tip60 over PCAF, p300 and GCN5. NU9056 induces apoptosis of prostate cancer cells.
性状
Solid-liquid mixture
体外研究(In Vitro)
NU9056 (17-36 μM; 24-96 hours) results in both caspase 3 and caspase 9 activation in a time- and concentration-dependent manner. NU9056 (2.5-40 μM; 2 hours) treatment results in decreased levels of acetylated histone H4K16, H3K14 and H4K8, targets for Tip60-mediated acetylation.NU9056 treatment also decreases androgen receptor, prostate specific antigen, p53 and p21 protein levels. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
The mice are injected with Nu9056 (2 μg/g) and the hippocampus is collected 1 h later. Tip60 inhibition reduces H2A.Z binding at the -1 nucleosome of Arc, and the +1 nucleosome of Arc and Syp. Additionally, Nu9056 increases acetylation at the -1 nucleosome of Fos, Tacstd2, and Gria4, and the +1 nucleosome of Gria4. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Pure form -20°C 3 years;4°C 2 years
参考文献
[1]. Kelly Coffey, et al. Characterisation of a Tip60 specific inhibitor, NU9056, in prostate cancer. PLoS One. 2012;7(10):e45539.[2]. Klotilda Narkaj, et al. Blocking H2A.Z Incorporation via Tip60 Inhibition Promotes Systems Consolidation of Fear Memory in Mice. eNeuro. 2018 Nov 8;5(5):ENEURO.0378-18.2018.
溶解度数据
In Vitro: DMSO : 125 mg/mL (537.94 mM; Need ultrasonic)配制储备液