名称 | Scriptaid |
描述 | Scriptaid (GCK1026) is an inhibitor of HDAC, and has a greater effect on acetylated H4 than H3. |
细胞实验 | Cells are plated at a cell density of 5000 cells/well in 12 well plates and treated with Scriptaid for up to 3 days. Cells numbers are counted daily using a Coulter counter.(Only for Reference) |
激酶实验 | Immunoblotting assay of histone acetylation: PANC-1 cells are treated with 2 μg/mL of Scriptaid for 18 h in culture medium. Treated and untreated cells are harvested with trypsin-EDTA, washed with PBS, and resuspended in a protein sample buffer. Protein concentration is determined by BCA protein assay reagents. Fifty μg of proteins from each sample is loaded on a 12% denaturing polyacrylamide gel. Proteins are subsequently transferred to a nylon membrane using MilliblotGraphite Electroblotter I. The nylon membrane is incubated with rabbit antihuman acetyl-lysine antibody, followed by goat antirabbit antibody coupled to horseradish peroxidase, developed with SuperSignal substrates, and detected by film. |
体外活性 | Scriptaid (6 μM) 在PANC-1细胞中导致组蛋白乙酰化增加超过100倍。Scriptaid (8 μM) 对PANC-1细胞无致死作用,并对MDAMB-468的影响有限(存活率80%)。Scriptaid能够独立于转录积极诱导因子,增加pCMVb、p6SBE-luc和p6MBE-luc的转录。它能够诱导由病毒(SV40和CMV)或人类(泛素c, UB6)启动子驱动的p6MBE-luc、pCMVb和pUB6/V5-LacZ高表达,这不依赖于增强子(SBE与MBE)、启动子类型(病毒与细胞)、报告基因产物(荧光素酶与b-半乳糖酶)或报告构件的整合状态。[1] Scriptaid促进体细胞核转移(SCNT)卵母细胞发展至囊胚阶段,并允许全期发展(分别为3.4%,4.2%,7.6%,6.8%和4.1%)的所有浓度(分别为50, 100, 250, 500和2000 nM)。Scriptaid以剂量依赖性方式改善克隆B6D2F1胚胎的全期发展,250 nM效果最大。Scriptaid使得克隆所有重要近交系小鼠品系,如C57BL/6、C3H/He、DBA/2和129/Sv成为可能。Scriptaid处理能够增强克隆胚胎中新合成的mRNA水平。250 nM Scriptaid处理最多48小时,不抑制ICSI受精胚胎的发展。[2] Scriptaid抑制T. gondii太子滋生,IC50为39 nM。Scriptaid (0.225 μM) 完全保护HS68单层免受T. gondii太子侵害。[3] 48小时的Scriptaid处理后,Scriptaid抑制ER阴性细胞系MDA-MB-231、MDA-MB-435和Hs578t的生长,IC50为0.5-1.0 μg/mL。1 μg/mL Scriptaid处理48小时,引起乙酰化H3和乙酰化H4组蛋白尾部蛋白的积累,并最大20,000倍增加ER mRNA转录。[4] |
体内活性 | Scriptaid 在1.5至5.5 mg/kg剂量下对模型中的中度TBI后伤口造成依剂量递减的效应,最大减小伤口大小45%。即使治疗延迟到伤后12小时,也能达到类似的保护效果。此保护作用对于运动和认知功能是长期的,因为在伤后35天还能检测到类似的改进。Scriptaid使存活神经元增加42%,以及在海马CA3区域和周边损伤皮层内,其过程的数目和长度增加。Scriptaid治疗预防了TBI引起的皮质和海马CA3区域神经元中磷酸化AKT (p-AKT) 和磷酸化磷酸酸和张力蛋白同源物被删除在染色体10上的 (p-PTEN) 的减少。[6] 在人类乳腺癌异种移植模型MDA-MB-231中,Scriptaid治疗(3.5 mg/kg)明显抑制肿瘤生长,减小肿瘤体积75%。[4] |
存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 40 mg/mL (122.57 mM)
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关键字 | Autophagy | HDAC | GCK-1026 | Inhibitor | GCK 1026 | Apoptosis | Scriptaid | Influenza Virus | Histone deacetylases | inhibit |
相关产品 | Guanidine hydrochloride | Naringin | Valproic Acid | L-Glutamic acid | Gefitinib | Hydroxychloroquine | Dextran sulfate sodium salt (MW 4500-5500) | Stavudine | Tributyrin | L-Ascorbic acid | Paeonol | Sodium 4-phenylbutyrate |
相关库 | 抑制剂库 | 抗乳腺癌化合物库 | 经典已知活性库 | 抗癌化合物库 | 已知活性化合物库 | 自噬库 | 组蛋白修饰化合物库 | 抗衰老化合物库 | 表观遗传库 | 抗病毒库 |