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HAT Inhibitor II Sale

(Synonyms: 组蛋白乙酰转移酶抑制剂II,Histone Acetyltransferase Inhibitor II) 目录号 : GC12009

An inhibitor of HAT p300

HAT Inhibitor II Chemical Structure

Cas No.:932749-62-7

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5mg
¥882.00
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10mg
¥1,208.00
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Sample solution is provided at 25 µL, 10mM.

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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.

Chemical Properties

Cas No. 932749-62-7 SDF
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 SMILES BrC1=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°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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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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