| Identification | Back Directory | [Name]
CAS:932749-62-7 | [CAS]
932749-62-7 | [Synonyms]
CAS:932749-62-7
HAT Inhibitor II
Histone Acetyltransferase Inhibitor II
Histone Acetyltransferase Inhibitor II (compound 2c)
Cyclohexanone, 2,6-bis[(3-bromo-4-hydroxyphenyl)methylene]- | [Molecular Formula]
C20H16Br2O3 | [MDL Number]
MFCD11655778 | [MOL File]
932749-62-7.mol | [Molecular Weight]
464.15 |
| Chemical Properties | Back Directory | [Melting point ]
201-202 °C(Solv: isopropanol (67-63-0); water (7732-18-5)) | [Boiling point ]
580.8±50.0 °C(Predicted) | [density ]
1.733±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
≤20mg/ml in ethanol;30mg/ml in DMSO;50mg/ml in dimethyl formamide | [form ]
crystalline solid | [pka]
7.89±0.35(Predicted) | [color ]
Light yellow to yellow | [InChI]
InChI=1S/C20H16Br2O3/c21-16-10-12(4-6-18(16)23)8-14-2-1-3-15(20(14)25)9-13-5-7-19(24)17(22)11-13/h4-11,23-24H,1-3H2 | [InChIKey]
YOLKEKNTCBWPSD-UHFFFAOYSA-N | [SMILES]
C1(=O)C(=CC2=CC=C(O)C(Br)=C2)CCCC1=CC1=CC=C(O)C(Br)=C1 |
| Hazard Information | Back Directory | [Uses]
Histone Acetyltransferase Inhibitor II is a selective, cell-permeable p300/CBP HAT inhibitor, which may be used in the treatement of cystic fibrosis. | [Biological Activity]
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]. | [IC 50]
CBP/p300 | [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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