Uses
Histone Acetyltransferase Inhibitor II is a selective, cell-permeable p300/CBP HAT inhibitor, which may be used in the treatement of cystic fibrosis.
Biological Activity
hat inhibitor ii, a cell-permeable bis-arylidene cyclohexanone compound, selectively inhibits the histone acetyltransferase p300/creb-binding protein (cbp) with an ic50 value of 5 μm. it affects gcn5 and pcaf acetyltransferases only at much higher concentrations.histone acetyltransferase p300, a ubiquitously expressed global transcriptional coactivator, plays critical roles in a wide variety of cellular phenomena, involving in cell cycle control, differentiation, and apoptosis.
in vitro
hat inhibitor ii dose-dependently suppressed the proliferation of u251, u87, hs683 and shg44 cells. in hat inhibitor ii-treated u251 and shg44 cells, cell cycle arrest at the g2/m phase was triggered by hat inhibitor ii, significant levels of apoptosis, apoptotic body formation and dna fragmentation were induced, and cleavage of caspase-3, caspase-9 and parp were caused. additionally, hat inhibitor ii upregulated 965 genes and downregulated 984 genes in hat inhibitor ii-treated u251 cells [1].
in vivo
c57bl/6j mice were intraperitoneally administrated with hat inhibitor ii at a dose of 185 μg/g for 15 min. in muscle early postmortem, hat inhibitor ii inhibited protein acetylation, which reduced amp-activated protein kinase activation induced increase in the total acetylated proteins as well as glycolytic rate [2].
References
[1]. xu, l., li, z., tao, y., li, r., fang, f., & zhao, h. et al. histone acetyltransferase inhibitor ii induces apoptosis in glioma cell lines via the p53 signaling pathway. journal of experimental & clinical cancer research. 2014; 33:108.
[2]. li, q., li, z., lou, a., wang, z., zhang, d., & shen, q. histone acetyltransferase inhibitors antagonize amp-activated protein kinase in postmortem glycolysis. asian-australasian journal of animal sciences. 2016; 30(6): 857-864.
