Selisistat (EX 527, SEN0014196) is a potent and selectiveSIRT1inhibitor withIC50of 38 nM in a cell-free assay, exhibits >200-fold selectivity against SIRT2 and SIRT3. Phase 2.
In vitro

EX 527 exhibits potently inhibitory effect against SIRT1 deacetylase activity in a concentration-dependent manner with an IC50 of 38 nM, displays much lower activity against SIRT2 and SIRT3 with IC50 values of 19.6 μM and 48.7 μM, respectively. EX 527 does not inhibit SIRT4-7 and class I/II HDAC activity at concentrations up to 100 μM. EX-527 alone (1 μM) has no detectable effect on the acetylation of p53 lysine 382 in NCI-H460 cells. EX-527 significantly increases the amount of acetylated p53 in NCI-H460 cells, human mammary epithelial cells, U-2 OS and MCF-7 cells subjected to genotoxic agents such as Etoposide, Doxorubicin, Hydroxyurea, and Hydrogen peroxide, which is more effective than that caused by Nicotinamide (5 mM). But surprisingly EX 527 does not result in detectable effects on p53-controled gene expression, cell survival, or cell proliferation. EX 527 causes a 90% increase in cell number of HCT116 cells after 7 days in the condition of 0.1% serum but not 10% serum, suggesting that SIRT1 is a significant regulator of cell proliferation during growth factor deprivation conditions. EX 527 abrogates resveratrol effects on glucose responses, and prevents resveratrol-induced up-regulation of Glut2, glucokinase, Pdx-1, and Tfam in INS-1E Cells, due to the opposite effect of EX 527 and resveratrol on SIRT1 deacetylase activity.

In vivo

Administration of EX 527 (~10 μg) to rats increases hypothalamic acetyl-p53 levels by inhibiting hypothalamic SIRT1 activity. Co-administration of EX 527 with ghrelin markedly blunts the orexigenic action of ghrelin by decreasing the pAMPK levels, increasing the ACC levels, and abolishing the higher expression of the transcription factors FoxO1, pCREB, and Bsx and the neuropeptides NPY and AgRP in the hypothalamic arcuate nucleus.
Cell Data

cell lines：C. albicans strain SC5314

Concentrations：Dissolved in DMSO, final concentration 1 μM

Incubation Time：48 or 72 hours

Powder Purity:≥99%

规格

英文别名

SEN0014196 | (S)-6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide

规格或纯度

Moligand™, 10mM in DMSO

英文名称

Selisistat (EX 527)

生化机理

Selisistat（EX 527，SEN0014196）是一种强效的选择性 SIRT1 抑制剂，在无细胞实验中的 IC50 为 38 nM，对 SIRT2 和 SIRT3 的选择性大于 200 倍。第二阶段

储存条件

-80℃储存

运输条件

特低温运输

作用类型

抑制剂

作用机制

sirtuin 1 抑制剂

名称和识别符

分子类型

小分子

Isomeric SMILES

C1CC(C2=C(C1)C3=C(N2)C=CC(=C3)Cl)C(=O)N

分子量

248.71

Reaxy-Rn

416178

Reaxys-RN link address

https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=416178&ln=

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高级数据

关联靶点（人）

SIRT2 Tchem NAD 依赖性蛋白去乙酰化酶 sirtuin-2(NAD-dependent protein deacetylase sirtuin-2) (3 活性数据)

点击查看靶蛋白信息： SIRT2

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

SIRT1 Tchem NAD 依赖性蛋白去乙酰化酶 sirtuin-1(NAD-dependent protein deacetylase sirtuin-1) (26 活性数据)

点击查看靶蛋白信息： SIRT1

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

化学和物理性质

溶解性

Solubility (25°C) In vitro DMSO: 67 mg/mL (198.06 mM); Ethanol: 17 mg/mL (50.25 mM); Water: Insoluble;

折光率

1.69

沸点

531.72°C/760mmHg

熔点

178°C

安全和危险性（GHS）

象形图

GHS06, GHS07

信号词

Danger

危险声明

H319: 引起严重眼睛刺激

H301: 吞咽会中毒

预防措施声明

P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。

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P321: 特殊处理（请参阅此标签上的...）。

P405: 密闭存放

P501: 将内容物/容器处理到。。。

P264: 处理后要彻底洗手。

P270: 使用本产品时，请勿进食、饮水或吸烟。

P330: 漱口

P264+P265: 处理后彻底洗手[和…]。不要触摸眼睛。

P301+P316: 如果吞咽：立即寻求紧急医疗救助。

P337+P317: 如果眼睛刺激持续：寻求医疗帮助。

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批号(Lot Number)	证书类型	货号
G2429108	分析证书	S408283

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