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品質等級
化驗
≥98% (HPLC)
形狀
powder
顏色
white to beige
溶解度
DMSO: >20 mg/mL
儲存溫度
2-8°C
SMILES 字串
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 密鑰
FUZYTVDVLBBXDL-UHFFFAOYSA-N
應用
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。
特點和優勢
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。
儲存類別代碼
11 - Combustible Solids
水污染物質分類(WGK)
WGK 3
其他客户在看
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
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
Cells, 8(1), 11-11 (2019)
The Journal of reproduction and development, 63(5), 455-461 (2017-06-13)
Resveratrol is a potent activator of NAD-dependent deacetyltransferase sirtuin-1 (SIRT1) and affects lipid metabolism and ATP generation in somatic cells. In the present study, the effects of supplementing culture medium with resveratrol on lipid metabolism, ATP generation, and cryosensitivity of
The Role of Sirt1 in Epileptogenesis
eNeuro, 4(1) (2017)
The protective effects of Resveratrol against radiation-induced intestinal injury
BMC Complementary and Alternative Medicine, 17(1), 410-410 (2017)
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