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HAT Inhibitor II (Synonyms: Histone Acetyltransferase Inhibitor II)

Catalog No.GC12009

HAT Inhibitor II (compound 2c) is a potent, selective and cell permeable p300 histone acetyltransferase inhibitor, with an IC50 of 5 μM. HAT Inhibitor II shows anti-acetylase activity in mammalian cells.

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HAT Inhibitor II Chemical Structure

Cas No.: 932749-62-7

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Sample solution is provided at 25 µL, 10mM.

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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].

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.

Chemical Properties

Cas No. 932749-62-7 SDF
Synonyms Histone Acetyltransferase Inhibitor II
Chemical Name 2,6-bis[(3-bromo-4-hydroxyphenyl)methylene]-cyclohexanone
Canonical SMILES BrC1=C(O)C=CC(/C=C2CCC/C(C\2=O)=C\C3=CC(Br)=C(O)C=C3)=C1
Formula C20H16Br2O3 M.Wt 464.2
Solubility ≤20mg/ml in ethanol;30mg/ml in DMSO;50mg/ml in dimethyl formamide Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.1542 mL 10.7712 mL 21.5424 mL
5 mM 0.4308 mL 2.1542 mL 4.3085 mL
10 mM 0.2154 mL 1.0771 mL 2.1542 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 15 reference(s) in Google Scholar.)

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