所有图片(1)
About This Item
经验公式（希尔记法）:
C13H13ClN2O
CAS号:
分子量:
248.71
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77
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质量水平
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。
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
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
The Role of Sirt1 in Epileptogenesis
Hall Alicia M, et al.
eNeuro, 4(1) (2017)
The protective effects of Resveratrol against radiation-induced intestinal injury
Zhang H, et al.
BMC Complementary and Alternative Medicine, 17(1), 410-410 (2017)
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