AGK2 | SIRT2 Inhibitor | AmBeed-信号通路专用抑制剂

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AGK2 {[allProObj[0].p_purity_real_show]}

货号：A480363

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.

AGK2 化学结构
CAS号：304896-28-4

AGK2 3D分子结构
CAS号：304896-28-4

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AGK2 纯度/质量文件产品仅供科研

货号：A480363 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Cell, 2024, 101755. Ambeed. [ A399663 ]; • EMBO J., 2024. Ambeed. [ A295334 ]; • JMC, 2024, 67(20): 18265-18289. Ambeed. [ A538667 , A341145 , A117430 , A172297 ]; • JMC, 2024. Ambeed. [ A210558 , A1518164 ]; • Cell Death Discov., 2024, 10, 436. Ambeed. [ A384235 ]; 更多 >

Sirtuin 亚型比较

产品名称	SIRT1 ↓ ↑	SIRT2 ↓ ↑	SIRT3 ↓ ↑	SIRT5 ↓ ↑	SIRT6 ↓ ↑	SIRT7 ↓ ↑	Sirtuin ↓ ↑	其他靶点	纯度
Selisistat	++++ SIRT1, IC50: 38 nM								99%+
Resveratrol	✔								98%
Inauhzin	✔							p53	99%+
Suramin sodium salt	+++ SirT1, IC50: 297 nM			++ SirT5, IC50: 22 μM					99%+
Salermide	✔								98%
Quercetin Dihydrate	✔								95%
Sirtinol	+ SIRT1, IC50: 131 μM	++ SIRT2, IC50: 38 μM							98%+
AGK2		+++ SIRT2, IC50: 3.5 μM							99%+
Tenovin-3		✔						p53	99%+
3-TYP	++++ SIRT1, IC50: 88 nM	++++ SIRT2, IC50: 92 nM	++++ SIRT3, IC50: 16 nM						95%
Tenovin-6	++ SIRT1, IC50: 21 μM	++ SIRT2, IC50: 10 μM	+ SIRT3, IC50: 67 μM					p53	99%+
SirReal2		+++ SIRT2, IC50: 140 nM							99%+
Thiomyristoyl		++++ SIRT2, IC50: 28 nM							99%+
Et-29				✔					98%
OSS_128167	+ SIRT1, IC50: 1578 μM	+ SIRT2, IC50: 751 μM			+ SIRT6, IC50: 89 μM				98%
SIRT7 inhibitor 97491						+++ SIRT7, IC50: 325 nM			97%
Nicotinamide							✔		99+%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

AGK2 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].

AGK2 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
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

AGK2 动物研究

Animal study

AGK2 notably decreases mortality and cytokine levels in the blood, including TNF-α and IL-6. Furthermore, AGK2 reduces the production of TNF-α and IL-6 in cultured splenocytes^[4].

AGK2 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.

AGK2 实验方案

计算器

存储液制备

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

AGK2 技术信息

CAS号	304896-28-4
分子式	C₂₃H₁₃Cl₂N₃O₂
分子量	434.274

别名
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C

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

AGK2 {[allProObj[0].p_purity_real_show]}

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AGK2 {[allProObj[0].p_purity_real_show]}

AGK2 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

AGK2 质控信息

AGK2 生物活性

AGK2 细胞研究

AGK2 动物研究

AGK2 参考文献

AGK2 实验方案

AGK2 技术信息

最近浏览的产品

大规格询价

摩尔计算器

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总药量计算器

工作液计算器

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临床研究

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