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AGK2
| 貨號 | IEP1064 | 售價（元） | 480 |
| 規(guī)格 | 1mg | CAS號 | 304896-28-4 |
- 產(chǎn)品簡介
- 相關(guān)產(chǎn)品
|
貨號 |
名稱 |
規(guī)格 |
價格 |
|
IEP1064-0001MG |
AGK2 |
1MG |
480 |
|
IEP1064-0005MG |
AGK2 |
5MG |
1568 |
|
IEP1064-0025MG |
AGK2 |
25MG |
5010 |
產(chǎn)品簡介:
AGK2是一種選擇性的SIRT2 抑制劑,IC50為3.5 μM。AGK2 抑制SIRT1 和SIRT3 的IC50 分別為30和91 μM [1,2]。
AGK2 (0.01-20 μM；24h)在體外抑制肥大細(xì)胞脫顆粒作用,AGK2 處理能夠減少RBL-2H3 細(xì)胞中β-己糖苷酶和組胺高水平的表達[3]。AGK2 (1-5 μM；24h) 通過抑制HeLa 細(xì)胞中HSF1 蛋白的穩(wěn)定性,抑制細(xì)胞的生長和遷移[4]。AGK2 對SIRT2 抑制可通過增強干細(xì)胞記憶(TSCM)反應(yīng),顯著增強卡介苗(BCG)的主要感染和結(jié)核病復(fù)發(fā)的療效[5]。
AGK2 (1 μmol/mice；i.p；26h) 能夠抑制LPS 處理小鼠腦組織中BV2 微膠質(zhì)細(xì)胞的活化和iNOS、SIRT2 的表達[6]。AGK2 (1μmol/mice；i.p；26h) 預(yù)處理可以降低ALF 肝臟組織中的促炎性細(xì)胞因子水平。AGK2 也能改善TAA 引起的生存率[7]。AGK2 (82 mg/kg；i.p；7days) 處理可以抑制HBV 轉(zhuǎn)基因小鼠血清中的HBV DNA、HBeAg 和HBsAg 水平,以及肝臟中的HBV DNA、RNA 和HBc 的表達[8]。
產(chǎn)品性質(zhì):
Cas No.:304896-28-4
別名:2-氰基-3-[5-(2,5-二氯苯基)-2-呋喃基]-N-5-喹啉基-2-丙烯酰胺
化學(xué)名:(E)-2-cyano-3-(5-(2,5-dichlorophenyl)furan-2-yl)-N-(quinolin-5-yl)acrylamide
Canonical SMILES:ClC(C(C1=CC=C(/C=C(C#N)/C(NC2=C3C(N=CC=C3)=CC=C2)=O)O1)=C4)=CC=C4Cl
分子式:C23H13Cl2N3O2
分子量:434.27
溶解度:≥ 9.3mg/mL in DMSO
儲存條件:Store at -20°C
注意事項:
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References:
[1]. Tatum PR, Sawada H, et,al. Identification of novel SIRT2-selective inhibitors using a click chemistry approach. Bioorg Med Chem Lett. 2014 Apr 15;24(8):1871-4. doi: 10.1016/j.bmcl.2014.03.026. Epub 2014 Mar 20. PMID: 24675380.
[2]. Outeiro TF, Kontopoulos E, et,al. Sirtuin 2 inhibitors rescue alpha-synuclein-mediated toxicity in models of Parkinson's disease. Science. 2007 Jul 27;317(5837):516-9. doi: 10.1126/science.1143780. Epub 2007 Jun 21. PMID: 17588900.
[3]. Kim YY, Hur G, et,al. AGK2 ameliorates mast cell-mediated allergic airway inflammation and fibrosis by inhibiting FcεRI/TGF-β signaling pathway. Pharmacol Res. 2020 Sep;159:105027. doi: 10.1016/j.phrs.2020.105027. Epub 2020 Jun 18. PMID: 32565308.
[4]. Kim HW, Kim SA, et,al. Sirtuin inhibitors, EX527 and AGK2, suppress cell migration by inhibiting HSF1 protein stability. Oncol Rep. 2016 Jan;35(1):235-42. doi: 10.3892/or.2015.4381. Epub 2015 Nov 2. PMID: 26530275.
[5]. Bhaskar A, Pahuja I, et,al. SIRT2 inhibition by AGK2 enhances mycobacteria-specific stem cell memory responses by modulating beta-catenin and glycolysis. iScience. 2023 Apr 10;26(5):106644. doi: 10.1016/j.isci.2023.106644. PMID: 37192966; PMCID: PMC10182326.
[6]. Jiao F, Wang Y, et,al. AGK2 Alleviates Lipopolysaccharide Induced Neuroinflammation through Regulation of Mitogen-Activated Protein Kinase Phosphatase-1. J Neuroimmune Pharmacol. 2020 Jun;15(2):196-208. doi: 10.1007/s11481-019-09890-x. Epub 2019 Nov 30. PMID: 31786712.
[7]. Jiao FZ, Wang Y, et,al. Protective role of AGK2 on thioacetamide-induced acute liver failure in mice. Life Sci. 2019 Aug 1;230:68-75. doi: 10.1016/j.lfs.2019.05.061. Epub 2019 May 23. PMID: 31129140.
[8]. Yu HB, Jiang H, et,al. 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.