NiCur 是一种有效的选择性CBP Histone Acetyltransferase (HAT)抑制剂,其IC50值为 0.35 μΜ。NiCur 阻断CBP HAT活性,下调基因毒性应激时 p53 的激活。 NiCur 可用于不影响靶蛋白表达的机制研究。
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NiCur is a potent and selective CBP histone acetyltransferase (HAT) inhibitor with an IC 50 value of 0.35 μΜ. NiCur, which blocks CBP HAT activity and downregulates p53 activation upon genotoxic stress. NiCur can be used for performing mechanistic studies without affecting the expression of target proteins [1].
体外活性
NiCur (0.5~1 μM; U2OS cells) reduces the Dox-induced p53K382ac, p53S15p, and p53 levels in a dose-dependent manner [1]. NiCur (1.5 μM) reduces the level of H3K27ac. NiCur (1.5 μM; U2OS cells) restores cellular proliferation. NiCur (Intestinal epithelial cells) down-regulates Dox-mediated p53 activation without affecting the levels of H2A.X S139p. NiCur can modulate the gene regulatory switch for reprogramming chromatin landscape. NiCur blocks CBP HAT activity [1]. Western Blot Analysis [1] Cell Line: U2OS cells Concentration: 0.5~1 μM Incubation Time: Result: Reduced the Dox-induced p53K382ac, p53S15p, and p53 levels in a dose-dependent manner.
分子式
C22H16N2O
分子量
324.38
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years