产品属性：
产品名称 | 规格 | CAS号 | 型号 |
AGK 2 | 10mM (in 1mL DMSO) 10mg 50mg | 304896-28-4 | EY-Y0165094 |
Cas No.304896-28-4
别名
化学名 (E)-2-cyano-3-(5-(2,5-dichlorophenyl)furan-2-yl)-N-(quinolin-5-yl)acrylamide
分子式 C23H13Cl2N3O2
分子量 434.27
溶解度 ≥ 9.3mg/mL in DMSO
储存条件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述：
AGK 2 is a potent and selective inhibitor of sirtuin 2 with IC50 value of 3.5 μM [1].
Sirtuin 2 (SIRT2) is a NAD-dependent deacetylase and is involved in cell cycle regulation through α-tubulin deacetylation. SIRT2 plays an important role in neuroprotective effects and the pathogenesis and development of cancer [1] [2] [3].
AGK 2 is a potent and selective SIRT2 inhibitor. AGK 2 inhibited SIRT2 with IC50 value of 3.5 μM and slightly inhibited SIRT1 and 3 at concentrations over 40 μM. AGK 2 increased acetylation of tubulin heterodimers from bovine brain. In HeLa cells expressing SIRT2-myc, AGK2 effectively inhibited SIRT2-myc activity. AGK2 also dose-dependently increased acetylated tubulin. In H4 cells transfected with α-Syn, AGK2 dose-dependently reduced α-Syn-mediated toxicity. In primary midbrain cultures transduced with lentivirus encoding α-SynA53T, AGK2 rescued dorsomedial neurons in a dose-dependent way [1]. In primary rat astrocytes, AGK-2 (35 μM) significantly inhibited astrocyte viability and proliferation and also inhibited astrocyte activation induced by beta amyloid 1-42 (Aβ 1-42). Also, AGK2 significantly inhibited the increase of iNOS and COX-2 induced by Aβ 1-42 [2]. In glioblastoma multiforme cancer stem cells (GBM CSCs), AGK-2 exhibited good antiproliferative activity [3].
References:
[1]. Outeiro TF, Kontopoulos E, Altmann SM, et al. Sirtuin 2 inhibitors rescue alpha-synuclein-mediated toxicity in models of Parkinson's disease. Science, 2007, 317(5837): 516-519.
[2]. Scuderi C, Stecca C, Bronzuoli MR, et al. Sirtuin modulators control reactive gliosis in an in vitro model of Alzheimer's disease. Front Pharmacol, 2014, 5: 89.
[3]. Rotili D, Tarantino D, Nebbioso A, et al. Discovery of salermide-related sirtuin inhibitors: binding mode studies and antiproliferative effects in cancer cells including cancer stem cells. J Med Chem, 2012, 55(24): 10937-10947.
关键字： 304896-28-4;C23H13Cl2N3O2;AGK 2;
上海一研生物科技有限公司Shanghai yiyan bio-technology Co. Ltd.主要从事免疫学、分子生物学和常规生化试剂等为一体的科研产品销售企业，公司自成立以来，秉承""全心全意服务于科研工作者""的企业理念，立足生物科技领域，运用生物技术和科研试剂，发展现代生物科技，为各类大中小医院及其它医疗机构、高等院校、科研院所、企事业单位提供优质的产品，服务生物科技领域的科学研究人员。
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