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Merck
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E7034

Sigma-Aldrich

EX-527

≥98% (HPLC)

别名:

6-氯-2，3，4，9-四氢-1H-咔唑-1-甲酰胺

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About This Item

经验公式（希尔记法）:
C13H13ClN2O
CAS号:
49843-98-3
分子量:
248.71
MDL编号:
MFCD03009471
UNSPSC代码:
12352200
PubChem化学物质编号:
329799003
NACRES:
NA.77

方案

≥98% (HPLC)

表单

powder

颜色

white to beige

溶解性

DMSO: >20 mg/mL

储存温度

2-8°C

SMILES字符串

NC(=O)C1CCCc2c1[nH]c3ccc(Cl)cc23

InChI

1S/C13H13ClN2O/c14-7-4-5-11-10(6-7)8-2-1-3-9(13(15)17)12(8)16-11/h4-6,9,16H,1-3H2,(H2,15,17)

InChI key

FUZYTVDVLBBXDL-UHFFFAOYSA-N

应用

EX-527用于：
  • 1％二甲基亚砜，30％ 聚乙二醇400和1％Tween 80中，通过处理C57BL/6N小鼠，以研究其对肠道形态变化和隐窝细胞凋亡的影响
  • 作为sirtuin 1的抑制剂，用于处理在Dulbecco′s改良Eagle′s培养基中培养的人癌症细胞系MCF-7（Michigan cancer foundation-7）和HCT116（结肠癌细胞系），以研究其对线粒体ATP（三磷酸腺苷）产生的影响
  • 脑室内注入大鼠癫痫发生模型，以获取海藻酸诱导的癫痫持续状态所刺激的sirtuin 1活性

生化/生理作用

EX-527是一种有效的选择性sirtuin 1（SIRT1）抑制剂 （IC50 38 nM），可从高通量筛选中鉴定出来。与SIRT2或SIRT3 相比，EX-527 对 SIRT1的选择性更高（200-500 倍），并且已经证明是一种使用H3K56 去乙酰化位点底物的有效 SIRT6抑制剂。EX-527在浓度高达 100uM 时不会抑制 I/II 类 HDAC 活性。 增强 p53 乙酰化以响应 DNA 损伤剂。EX-527是外消旋的；活性异构体（EX-243）给出类似的结果和效力，而另一种异构体（称为EX-242）是无活性的。
有效的SIRT1和SIRT6抑制剂。

特点和优势

该化合物是基因调控研究的推荐产品。点击此处查看更多特色基因调控产品。在sigma.com/discover-bsm 上了解有关生物活性小分子在其他研究领域的更多信息。

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说明
价格

储存分类代码

11 - Combustible Solids

WGK

WGK 3

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000360630
0000360630
0000311779
0000053628
0000053627

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Ayana N Martin et al.
Journal of immunology research, 2018, 2402593-2402593 (2018-08-03)
Resistance and tolerance to infection are two universal fitness and survival strategies used by inflammation and immunity in organisms and cells to guard homeostasis. During sepsis, however, both strategies fail, and animal and human victims often die from combined innate
The Role of Sirt1 in Epileptogenesis
Hall Alicia M, et al.
eNeuro, 4(1) (2017)
Shuangdong Chen et al.
Biochemical and biophysical research communications, 516(4), 1196-1203 (2019-07-13)
Sirtuin1 (SIRT1), which is regulated by microRNA-34a (miR-34a), can modulate pathophysiology processes, including nonalcoholic fatty liver disease and intestinal ischemia/reperfusion injury. We previously reported that SIRT1, an NAD+-dependent deacetylase, plays a vital role in the development of neuropathic pain. However
A Rise in ATP, ROS, and Mitochondrial Content upon Glucose Withdrawal Correlates with a Dysregulated Mitochondria Turnover Mediated by the Activation of the Protein Deacetylase SIRT1
Song S and Hwang E
Cells, 8(1), 11-11 (2019)
Hong-Xia Liu et al.
Experimental cell research, 357(2), 271-281 (2017-05-30)
Mitochondrial trifunctional protein α-subunit (MTPα) is involved in the fatty acid β-oxidation (FAO) pathway. Two MTPα activities, 3-hydroxyacyl-CoA dehydrogenase and long-chain hydratase, have been linked with the occurrence and development of obesity and obesity-related disorders. These activities catalyze two steps
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