NiCur is a potent and selective CBP histone acetyltransferase (HAT) inhibitor with an IC50 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].
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].
[1]. Vincek AS, et al. Inhibitor of CBP Histone Acetyltransferase Downregulates p53 Activation and Facilitates Methylation at Lysine 27 on Histone H3. Molecules. 2018;23(8):1930. Published 2018 Aug 2.