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HAT Inhibitor II
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
HAT Inhibitor II图片
CAS NO:932749-62-7
包装与价格：
包装价格(元)
5mg电议
10mg电议

产品介绍
HAT Inhibitor II (compound 2c) 是一种有效的、选择性的和细胞可渗透的 p300 组蛋白乙酰转移酶抑制剂，IC50 为 5 μM. HAT Inhibitor II 在哺乳动物细胞中显示出抗乙酰化酶活性。
Cas No.932749-62-7
别名组蛋白乙酰转移酶抑制剂II,Histone Acetyltransferase Inhibitor II
化学名2,6-bis[(3-bromo-4-hydroxyphenyl)methylene]-cyclohexanone
Canonical SMILESBrC1=C(O)C=CC(/C=C2CCC/C(C\2=O)=C\C3=CC(Br)=C(O)C=C3)=C1
分子式C20H16Br2O3
分子量464.2
溶解度≤20mg/ml in ethanol;30mg/ml in DMSO;50mg/ml in dimethyl formamide
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.