- 抑制劑
- 化合物庫
- 抗體
- 生物試劑
- 新產(chǎn)品
- 聯(lián)系我們
AGK2
AGK2是一個有效的選擇性SIRT2抑制劑，IC50值為3.5 μM。對其他如SIRT1或SIRT3的抑制作用，在10倍以上的濃度時仍很微弱。
AGK2 Chemical Structure
CAS: 304896-28-4
產(chǎn)品質(zhì)控
批次：
純度：
99.98%
99.98
AGK2相關(guān)產(chǎn)品
| 相關(guān)靶點 | SIRT1 SIRT2 SIRT3 SIRT6 SIRT5 | 點擊展開 |
|---|---|---|
| 相關(guān)產(chǎn)品 | Selisistat (EX 527) SRT1720 HCl Sirtinol Quercetin Fisetin 3-TYP OSS_128167 SRT2104 (GSK2245840) SirReal2 Thiomyristoyl Salvianolic acid B SRT2183 UBCS039 Salermide SRT3025 HCl AK 7 NRD167 Inauhzin CAY10602 | 點擊展開 |
| 相關(guān)化合物庫 | 激酶抑制劑庫 血管生成相關(guān)化合物庫 TGF-beta/Smad信號通路庫 細胞骨架信號通路化合物庫 抗心血管疾病化合物庫 | 點擊展開 |
相關(guān)信號通路圖
細胞實驗數(shù)據(jù)示例
| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
|---|---|---|---|---|---|
| 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 | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | AGK2是一個有效的選擇性SIRT2抑制劑，IC50值為3.5 μM。對其他如SIRT1或SIRT3的抑制作用，在10倍以上的濃度時仍很微弱。 | ||
|---|---|---|---|
| 靶點 |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | 在SIRT2-myc表達的HeLa細胞，AGK2有效抑制SIRT2的活性，并增加乙?；奈⒐艿鞍?。在初級中腦培養(yǎng)基中，AGK2保護多巴胺能神經(jīng)元免受α-Syn引起的毒性。[1] AGK2誘導(dǎo)C6膠質(zhì)瘤細胞中細胞壞死和caspase-3依賴性細胞凋亡。[2] SIRT2也能減少merlin突變型小鼠schwann細胞(MSCs)的生存能力，而基本不降低野生型MSC生存能力。[3] | |||
|---|---|---|---|---|
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | 在帕金森氏病的果蠅模型中，AGK2清除α-Syn介導(dǎo)的毒性并修正聚合。[1] | |
|---|---|---|
| 動物實驗 | Animal Models | 帕金森氏病的果蠅模型 |
| Dosages | 1mM | |
| Administration | -- | |
化學(xué)信息&溶解度
| 分子量 | 434.27 | 分子式 | C23H13Cl2N3O2 |
| CAS號 | 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 | ||
| 儲存條件(自收到貨起) | |||
|
體外溶解度 |
DMSO : 10 mg/mL ( (23.02 mM) Warmed with 50°C water bath; Ultrasonicated; ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Water : Insoluble Ethanol : Insoluble |
摩爾濃度計算器 |
|
體內(nèi)溶解度 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 | ||||
實驗計算
動物體內(nèi)配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
技術(shù)支持
在訂購、運輸、儲存和使用我們的產(chǎn)品的任何階段，您遇到的任何問題，均可以通過撥打我們的熱線電話400-668-6834，或者技術(shù)支持郵箱tech@selleck.cn，直接聯(lián)系到我們。我們會在24小時內(nèi)盡快聯(lián)系您。
如果有其他問題，請給我們留言。
* 必填項
Tags: buy AGK2 | AGK2 supplier | purchase AGK2 | AGK2 cost | AGK2 manufacturer | order AGK2 | AGK2 distributor
