Selisistat

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Chemical Structure| 49843-98-3 同义名 : 司来司他 ;EX-527; SEN0014196; (±)-EX-527
CAS号 : 49843-98-3
货号 : A142021
分子式 : C13H13ClN2O
纯度 : 99%+
分子量 : 248.71
MDL号 : MFCD03009471
存储条件：

Pure form Sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(422.18 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
靶点

  • SIRT1

    SIRT1, IC50:38 nM
描述 Selisistat (EX-527) is a potent and selective SirT1 (Sir2 in Drosophila melanogaster) inhibitor with an IC50 of 123 nM for SirT1, which alleviates pathology in multiple animal and cell models of Huntington's disease[1].[2].
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
HEK 293 Growth Inhibition Assay 24 h IC50=97.7 ± 8.1 μM 24998427
HEK 293 Growth Inhibition Assay 48 h IC50=69.0 ± 0.7 μM 24998427
HeLa Growth Inhibition Assay 24 h IC50=37.9 ± 1.8 μM 24998427
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.02mL

0.80mL

0.40mL

20.10mL

4.02mL

2.01mL

40.21mL

8.04mL

4.02mL
参考文献

[1]Smith MR, et al. A potent and selective Sirtuin 1 inhibitor alleviates pathology in multiple animal and cell models of Huntington's disease. Hum Mol Genet. 2014;23(11):2995-3007.

[2]Napper AD, et al. Discovery of indoles as potent and selective inhibitors of the deacetylase SIRT1 [published correction appears in J Med Chem. 2007 Mar 8;50(5):1086]. J Med Chem. 2005;48(25):8045-8054.