304896-28-4|AGK2|CsnPharm

CAS No.: 304896-28-4

AGK2 Catalog No. CSN13831

Synonyms: AGK2

AGK2 is a potent, and selective SIRT2 inhibitor with IC50 of 3.5 μM that minimally affects either SIRT1 or SIRT3 at 10-fold higher levels.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述AGK2 is a selective Sirt2 inhibitor with IC50 value of 3.5 μM (measured by SIRT2 enzymatic assay) with almost no activity against SIRT1 and SIRT3 up to 40μM. AGK2 is usually used in research of neuroprotection. Inhibition of Sirt2 by AGK2 at concentration of 10μM reducedα-Syn–mediated toxicity in cells. Administration of AGK2 at concentration of 500μM or 1000μM rescued α-Syn–mediated toxicity of dorsomedial dopamine neurons in a Drosophila PD model. Increased level of acetylated tubulin could be observed after treatment with AGK2. Treatment with AGK2 at concentration of 10μM for 6h could exacerbate H2O2 (0.5 or 1mM)-induced decreases in the intracellular ATP level in PC12 cells. Addition of 10μM AGK2 moderately increased the percentage of high-ploidy megakaryocytic cells.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
Escherichia coli BL21 (DE3) cells	-	Function assay	-	Inhibition of full length human SIRT2 expressed in Escherichia coli BL21 (DE3) cells using fluorogenic 7-amino-4-methylcoumarin (AMC)-labeled peptide by fluorescence assay, IC50=1.56 μM	25275824
H4 cells	-	Function assay	24 h	Inhibition of SIRT2 in H4 cells co-transfected with alphaSyn and synphilin1 assessed as enlarged alphaSyn inclusions after 24 hrs	17588900
HeLa cells	-	Function assay	-	Inhibition of over-expressed SIRT2 immunoprecipitated from HeLa cells transfected with SIRT2-myc expression construct	17588900

更多
动物研究
剂量
Mice: 15 mg/kg^[3] (i.v.); 10 mg/kg^[4] (i.p.), 82 mg/kg^[5] (i.p.)

给药途径
i.v., i.p.
参考文献

动物研究
剂量	Mice: 15 mg/kg^[3] (i.v.); 10 mg/kg^[4] (i.p.), 82 mg/kg^[5] (i.p.)
给药途径	i.v., i.p.

[1] He X, Nie H, et al. SIRT2 activity is required for the survival of C6 glioma cells. Biochem Biophys Res Commun. 2012 Jan 6;417(1):468-72.
[2] Outeiro TF, Kontopoulos E, et al. Sirtuin 2 inhibitors rescue alpha-synuclein-mediated toxicity in models of Parkinson's disease. Science. 2007 Jul 27;317(5837):516-9. Epub 2007 Jun 21.

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
- 2.3027 mL
- 11.5135 mL
- 23.0269 mL
- 5 mM
- 0.4605 mL
- 2.3027 mL
- 4.6054 mL
- 10 mM
- 0.2303 mL
- 1.1513 mL
- 2.3027 mL

技术信息

CAS号

304896-28-4

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C23H13Cl2N3O2

运输

蓝冰

分子量

434.27

别名

AGK2

溶解度

DMSO	15.0 mg/mL (34.5 mM) warming
Water	insoluble

动物实验配方

8% DMSO+30% PEG 300+water

1.4 mg/mL

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Escherichia coli BL21 (DE3) cells	-	Function assay	-	Inhibition of full length human SIRT2 expressed in Escherichia coli BL21 (DE3) cells using fluorogenic 7-amino-4-methylcoumarin (AMC)-labeled peptide by fluorescence assay, IC50=1.56 μM	25275824
H4 cells	-	Function assay	24 h	Inhibition of SIRT2 in H4 cells co-transfected with alphaSyn and synphilin1 assessed as enlarged alphaSyn inclusions after 24 hrs	17588900
HeLa cells	-	Function assay	-	Inhibition of over-expressed SIRT2 immunoprecipitated from HeLa cells transfected with SIRT2-myc expression construct	17588900
human 30P cells	-	Cytotoxic assay	72 h	Cytotoxicity against human 30P cells after 72 hrs by celltiter-glo luminescent assay, CC50=12.5 μM	23189967
human 30PT cells	-	Cytotoxic assay	72 h	Cytotoxicity against human 30PT cells after 72 hrs by Cell-titer GLo assay, CC50=9.6 μM	22931526
human HCT116 cells	10 μM	Function assay	8 h	Inhibition of SIRT2 in human HCT116 cells assessed as increase in acetylated alpha-tubulin at 10 uM after 8 hrs by Western blot analysis	22642300

AGK2 Catalog No. CSN13831

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