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AGK2

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Chemical Structure| 304896-28-4 同义名 : -
CAS号 : 304896-28-4
货号 : A480363
分子式 : C23H13Cl2N3O2
纯度 : 99%+
分子量 : 434.274
MDL号 : MFCD01909444
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 12 mg/mL(27.63 mM)，配合低频超声助溶，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
动物实验配方：

8% DMSO+30% PEG 300+water 1.4 mg/mL

生物活性
靶点

  • SIRT2

    SIRT2, IC50:3.5 μM
描述 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].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 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
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.30mL

0.46mL

0.23mL

11.51mL

2.30mL

1.15mL

23.03mL

4.61mL

2.30mL
参考文献

[1]Yu HB, Jiang H, Cheng ST, Hu ZW, Ren JH, Chen J. AGK2, A SIRT2 Inhibitor, Inhibits Hepatitis B Virus Replication In Vitro And In Vivo. Int J Med Sci. 2018 Sep 7;15(12):1356-1364. doi: 10.7150/ijms.26125. PMID: 30275764; PMCID: PMC6158674.

[2]Kim HW, et al. Sirtuin inhibitors, EX527 and AGK2, suppress cell migration by inhibiting HSF1 protein stability. Oncol Rep. 2016 Jan;35(1):235-42.

[3]Li Y, et al. Poly(ADP-ribose) polymerase mediates both cell death and ATP decreases in SIRT2 inhibitor AGK2-treated microglial BV2 cells. Neurosci Lett. 2013 Jun 7;544:36-40.

[4]Zhao T, et al. Selective Inhibition of SIRT2 Improves Outcomes in a Lethal Septic Model. Curr Mol Med. 2015;15(7):634-41.