|6-氯-2,3,4,9-四氢-1H-咔唑-1-甲酰胺|CsnPharm

CAS No.: 49843-98-3

Selisistat/6-氯-2,3,4,9-四氢-1H-咔唑-1-甲酰胺 Catalog No. CSN10146

Synonyms: SEN0014196;EX-527

EX-527 is a potent and selective SIRT1 inhibitor with IC50 of 38 nM, exhibits > 200-fold selectivity against SIRT2 and SIRT3.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Sirtuin 1

IC50:38nM
描述SIRT1 is an enzyme which can remove acetyl groups without hydrolysis of NAD⁺ and can deacetylate p53 to modulate its function such as DNA damage-induced cell death. EX-527 is a novel, potent, and specific inhibitor of SIRT1 catalytic activity with IC50 value of 38nM (measure by activity of GST-tagged human SIRT1 purified from 293T cells), almost no activity to SIRT2 (IC50=19.6μM) or SIRT3 (IC50=48.7μM). Treatment with 1μM EX-527 for 6h after DNA damage by etoposide could enhance the level of p53 acetylation on K382 site in NCI-H460 cells. And this inhibition of SIRT1 catalytic activity by EX-527 could also be observed after treatment with adriamycin, hydroxyurea, or hydrogen peroxide in NCI-H460 cells, or in U-2 OS, MCF-7 and HMEC treated with etoposide. However, p53-controlled gene expression, such as p21, as well as cell survival or proliferation are not altered by inhibition of SIRT1 through EX-527 in these p53-positive cell lines. Inhibition of Sirt by EX-527 induced apoptosis-like changes in blood platelets, associated with a rise in active Bax and a significant drop in platelet count. Administration of 20mg/kg EX-527 led to a reduction in the number of reticulated platelets and thrombocytopenia in mice.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

动物研究

剂量

Mice: 10 mg/kg^[3] (i.p.); 5 mg/kg - 100 mg/kg^[4] (p.o.); 20 mg/kg25829495 (i.v.)

给药途径

i.p., p.o., i.v.

动物药代数据

Animal	Mice^[4]
Dose	20 mg/kg
Administration	p.o.
C_ss	3.2 ± 0.4 µM
T_1/2	0.9 ± 0.2 h
AUC_0→last	77.5 ± 9.7 µM·h
T_max	0.50 ± 0.0 h
C_max	29.3 ± 6.4 µM

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 4.0208 mL
- 20.1039 mL
- 40.2078 mL
- 5 mM
- 0.8042 mL
- 4.0208 mL
- 8.0416 mL
- 10 mM
- 0.4021 mL
- 2.0104 mL
- 4.0208 mL

技术信息

CAS号

49843-98-3

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C13H13ClN2O

运输

蓝冰

分子量

248.71

别名

SEN0014196;EX-527

溶解度

DMSO	49.0 mg/mL (197.0 mM)
Water	Insoluble
Ethanol	16.0 mg/mL (64.3 mM)

动物实验配方

5% DMSO +30% PEG400+2% tween80+H2O

10 mg/mL

clear

大规格询价

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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
HeLa	-	Growth Inhibition Assay	48 h	IC50=8.9 ± 1.9 μM	24998427
HUVECs	10 μM	Apoptosis Assay	24 h	bolishes the protective effect of resveratrol in cell viability	23358928
INS-1E	1 μm	Function Assay	24 h	prevents resveratrol-induced up-regulation of Glut2, glucokinase,Pdx-1, and Tfam	21163946
K562	0.1-1 μM	Function Assay	2 h	stimulates Nrf2-dependent gene transcription	21196497
MCF-7	0-100 μM	Growth Inhibition Assay	24/48/72 h	represses cell proliferation at the concentration ≥100 μM	20371709
NCI-H460	1 μm	Function Assay	6 h	produces a concentration-dependent increase in the amount of acetylated p53	16354677
Platelets	10/50 μM	Apoptosis Assay	10 min	increases ROS level in a dose-dependent manner	25829495
RMECs	10 μM	Apoptosis Assay	24 h	attenuates the anti-apoptotic effect of Des-G	24486147

Selisistat/6-氯-2,3,4,9-四氢-1H-咔唑-1-甲酰胺 Catalog No. CSN10146

靶点选择性

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