AGK2 acts as a selective inhibitor for SIRT2, demonstrating an IC50 value of 3.5 μM. It also inhibits SIRT1 and SIRT3, with respective IC50 values of 30 μM and 91 μM[1]. AGK2 markedly suppresses cell multiplication in correlation with the dosage. Additionally, AGK2 curtails cell expansion dose-dependently while not triggering cytotoxic effects at lower concentrations. Following a 12-day period of AGK2 treatment at 5 μM, there is a notable decline in the colony-forming capability of cells in soft agar to 46% compared to control cells. Western blot results indicate a dose-dependent reduction in the levels of CDK4, CDK6, and cyclin D1 post-AGK2 treatment. AGK2 also downregulates the expression of the p53 protein[2]. Exposing microglial BV2 cells to AGK2 at a concentration of 10 μM results in a considerable elevation of PAR signals. This treatment also causes a notable reduction in intracellular ATP levels and a significant rise in both advanced apoptosis and cell necrosis[3].
AGK2 细胞研究
细胞系
浓度
检测类型
检测时间
活性说明
数据源
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
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
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