Name: HAT Inhibitor II
Price: 280.00 USD

- Overview
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    Background
    
    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].
    
    [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.
- Properties
  - Alternative Name
    
    Histone Acetyltransferase Inhibitor II; 2,6-bis[(3-bromo-4-hydroxyphenyl)methylene]-cyclohexanone
    
    CAS Number
    
    932749-62-7
    
    Molecular Formula
    
    C20H16Br2O3
    
    Molecular Weight
    
    464.2
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≤20mg/ml in ethanol;30mg/ml in DMSO;50mg/ml in dimethyl formamide
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only