化合物Scriptaid T6980

Product Introduction
Bioactivity


英文名: Scriptaid

描述: Scriptaid (GCK1026) 是一种组蛋白去乙酰化酶抑制剂，也是抗病毒药的敏化剂。它可研究癌症，与爱泼斯坦-巴尔病毒相关的淋巴瘤。

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 elicits a dose-dependent decrease in lesion size (a maximal decrease of 45%) at 1.5 to 5.5 mg/kg and a concomitant attenuation in motor and cognitive deficits when delivered 30 minutes postinjury in a model of mode rate TBI. Comparable protection is achieved even when treatment is delayed to 12 h postinjury. The protection of motor and cognitive functions is long lasting, as similar improvements are detected 35 days postinjury. Scriptaid induces an increase in surviving neurons (42%), as well as the number/length of their processes within the CA3 region of the hippocampus and the pericontusional cortex. Scriptaid treatment prevents the decrease in phospho-AKT (p-AKT) and phosphorylated phosphatase and tensin homolog deleted on chromosome 10 ( p-PTEN) induced by TBI in cortical and CA3 hippocampal neurons. [6] Scriptaid treatment (3.5 mg/kg) clearly inhibits tumor growth in a human breast cancer xenograft MDA-MB-231 model, reducing tumor volume by 75%. [4]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 32.6 mg/mL (100 mM)


关键字: Autophagy | HDAC | GCK-1026 | Inhibitor | GCK 1026 | Apoptosis | Scriptaid | Influenza Virus | Histone deacetylases | inhibit

相关产品: MI-3 | Ethyl pyruvate | BI-847325 | (E)-Flavokawain A | Selonsertib | STF-118804 | Diosgenin glucoside | Ramipril | Nystatin | Cinobufagin

相关库: Anti-Aging Compound Library | Anti-Breast Cancer Compound Library | NF-κB Signaling Compound Library | Cancer Cell Differentiation Compound Library | Inhibitor Library | Hematonosis Compound Library | DNA Damage & Repair Compound Library | Anti-Pancreatic Cancer Compound Library | Autophagy Compound Library | NO PAINS Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途