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- qPCR
- 2x SYBR Green qPCR Master Mix
- 2x SYBR Green qPCR Master Mix(Low ROX)
- 2x SYBR Green qPCR Master Mix(High ROX)
- 蛋白實驗
- Protein A/G免疫沉淀磁珠
- Anti-DYKDDDDK Tag免疫磁珠
- Anti-DYKDDDDK Tag親和凝膠
- Anti-Myc免疫磁珠
- Anti-HA免疫磁珠
- 磁力架
- Poly DYKDDDDK Tag多肽
- 細(xì)胞核與細(xì)胞漿蛋白抽提試劑盒
- 免疫磁珠
- 蛋白酶抑制劑Cocktail
- 蛋白酶抑制劑Cocktail(DMSO儲液)
- 磷酸酶抑制劑Cocktail
- 細(xì)胞實驗
- Cell Counting Kit-8 (CCK-8)
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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 3-TYP OSS_128167 SRT2104 (GSK2245840) SirReal2 Thiomyristoyl Salvianolic acid B SRT2183 UBCS039 Salermide SRT3025 HCl AK 7 Inauhzin NRD167 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(xì)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(xì)胞實驗數(shù)據(jù)示例
| 細(xì)胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻(xiàn)信息(PMID) |
|---|---|---|---|---|---|
| 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(xì)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 |
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| 體外研究(In Vitro) | ||||
| 體外研究活性 | 在SIRT2-myc表達(dá)的HeLa細(xì)胞，AGK2有效抑制SIRT2的活性，并增加乙酰化的微管蛋白。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(xì)胞中細(xì)胞壞死和caspase-3依賴性細(xì)胞凋亡。[2] SIRT2也能減少merlin突變型小鼠schwann細(xì)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) | |||
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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 |
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體內(nèi)溶解配方 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。
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