| CAS NO: | 932749-62-7 |
| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 464.2 |
| Cas No. | 932749-62-7 |
| Formula | C20H16Br2O3 |
| Synonyms | Histone Acetyltransferase Inhibitor II |
| Solubility | ≤20mg/ml in ethanol;30mg/ml in DMSO;50mg/ml in dimethyl formamide |
| 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 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
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.
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