AGK2
AGK2是一个有效的选择性SIRT2抑制剂，IC50值为3.5 μM。对其他如SIRT1或SIRT3的抑制作用，在10倍以上的浓度时仍很微弱。
AGK2 Chemical Structure
CAS: 304896-28-4
产品质控
批次：
纯度：
99.98%
99.98
AGK2相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| HCT116 | Function assay | 10 uM | 8 hrs | 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 |
| SH-SY5Y | Neuroprotective assay | 1 to 10 uM | 30 mins | Neuroprotective activity against oligomeric alpha-synuclein-induced cytotoxicity in human SH-SY5Y cells assessed as increase in cell growth at 1 to 10 uM preincubated for 30 mins followed by alpha-synuclein addition measured after 72 hrs by MTT assay | 26982234 |
| MCF7 | Function assay | 10 to 50 uM | 24 hrs | Inhibition of SIRT2 in human MCF7 cells assessed as increase in alpha-tubulin K40 acetylation level at 10 to 50 uM after 24 hrs in presence of TSA by Western blot analysis | 28135086 |
| H4 | Function assay | 24 hrs | Inhibition of SIRT2 in H4 cells co-transfected with alphaSyn and synphilin1 assessed as enlarged alphaSyn inclusions after 24 hrs | 17588900 | |
| 30PT | Cytotoxicity assay | 72 hrs | Cytotoxicity against human 30PT cells after 72 hrs by Cell-titer GLo assay, CC50=9.6μM | 22931526 | |
| 30P | Cytotoxicity assay | 72 hrs | Cytotoxicity against human 30P cells after 72 hrs by Cell-titer GLo assay, CC50=12.5μM | 22931526 | |
| 30PT | Cytotoxicity assay | 72 hrs | Cytotoxicity against human 30PT cells after 72 hrs by celltiter-glo luminescent assay, CC50=9.6μM | 23189967 | |
| 30P | Cytotoxicity assay | 72 hrs | Cytotoxicity against human 30P cells after 72 hrs by celltiter-glo luminescent assay, CC50=12.5μM | 23189967 | |
| U373 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human U373 cells after 72 hrs by MTT assay, IC50=47.6μM | 28475330 | |
| Hs683 | Cell cycle assay | 24 to 48 hrs | Cell cycle arrest in human Hs683 cells assessed as accumulation at sub-G1 phase at IC50 for MTT assay after 24 to 48 hrs by propidium iodide staining-based flow cytometry | 28475330 | |
| U373 | Cell cycle assay | 24 to 48 hrs | Cell cycle arrest in human U373 cells assessed as accumulation at sub-G1 phase at IC50 for MTT assay after 24 to 48 hrs by propidium iodide staining-based flow cytometry | 28475330 | |
| Hs683 | Cell cycle assay | 24 to 48 hrs | Cell cycle arrest in human Hs683 cells assessed as accumulation at G2/M phase at IC50 after 24 to 48 hrs by propidium iodide staining-based flow cytometry | 28475330 | |
| U373 | Cell cycle assay | 24 to 48 hrs | Cell cycle arrest in human U373 cells assessed as accumulation at G2/M phase at IC50 after 24 to 48 hrs by propidium iodide staining-based flow cytometry | 28475330 | |
| rat embryo midbrain | Function assay | Protection of dopaminergic cell death in rat embryo midbrain transduced with lentivirus encoding alphaSyn-A53T mutant assessed as tyrosine hydroxylase positive cells | 17588900 | ||
| HeLa | Function assay | Inhibition of over-expressed SIRT2 immunoprecipitated from HeLa cells transfected with SIRT2-myc expression construct | 17588900 | ||
| Escherichia coli cells | Function assay | Inhibition of human recombinant SIRT2 expressed in Escherichia coli cells using acetylated Lys side chain amino acids 379-382 (Arg-His-Lys-Lys(Ac)) p53 conjugated with aminomethylcoumarin as substrate by fluorescence assay, IC50=5.5μM | 22931526 | ||
| Escherichia coli cells | Function assay | Inhibition of human recombinant SIRT1 expressed in Escherichia coli cells using acetylated Lys side chain amino acids 379-382 (Arg-His-Lys-Lys(Ac)) p53 conjugated with aminomethylcoumarin as substrate by fluorescence assay, IC50=38μM | 22931526 | ||
| Escherichia coli BL21 (DE3) | 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=1.56μM | 25275824 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | AGK2是一个有效的选择性SIRT2抑制剂，IC50值为3.5 μM。对其他如SIRT1或SIRT3的抑制作用，在10倍以上的浓度时仍很微弱。 | ||
|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | 在SIRT2-myc表达的HeLa细胞，AGK2有效抑制SIRT2的活性，并增加乙酰化的微管蛋白。在初级中脑培养基中，AGK2保护多巴胺能神经元免受α-Syn引起的毒性。[1] AGK2诱导C6胶质瘤细胞中细胞坏死和caspase-3依赖性细胞凋亡。[2] SIRT2也能减少merlin突变型小鼠schwann细胞(MSCs)的生存能力，而基本不降低野生型MSC生存能力。[3] | |||
|---|---|---|---|---|
| 体内研究(In Vivo) | ||
| 体内研究活性 | 在帕金森氏病的果蝇模型中，AGK2清除α-Syn介导的毒性并修正聚合。[1] | |
|---|---|---|
| 动物实验 | Animal Models | 帕金森氏病的果蝇模型 |
| Dosages | 1mM | |
| Administration | -- | |
化学信息&溶解度
| 分子量 | 434.27 | 分子式 | C23H13Cl2N3O2 |
| CAS号 | 304896-28-4 | SDF | Download AGK2 SDF |
| Smiles | C1=CC2=C(C=CC=N2)C(=C1)NC(=O)C(=CC3=CC=C(O3)C4=C(C=CC(=C4)Cl)Cl)C#N | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 10 mg/mL ( (23.02 mM) Warmed with 50°C water bath; Ultrasonicated; ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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