Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Crebinostat 是一种有效的组蛋白去乙酰化酶 (HDAC) 抑制剂,对 HDAC1、HDAC2、HDAC3 和 HDAC6 有抑制作用, IC50 分别为 0.7 nM、1.0 nM、2.0 nM 和 9.3 nM。Crebinostat 可增加在体外神经元的突触蛋白 1 斑点沿树突 (synapsin-1 punctae along dendrites) 的密度。Crebinostat 可调节染色质介导的神经可塑性,增强小鼠的记忆。Crebinostat 可诱导组蛋白 H3 和组蛋白 H4 乙酰化,并增强 cAMP 反应元件结合蛋白 (CREB) 靶基因 Egr1 的表达。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,730 | 现货 | ||
5 mg | ¥ 4,290 | 现货 | ||
10 mg | ¥ 5,930 | 现货 | ||
25 mg | ¥ 8,980 | 现货 | ||
50 mg | ¥ 11,900 | 现货 | ||
100 mg | ¥ 16,300 | 现货 |
产品描述 | Crebinostat is a potent histone deacetylase (HDAC) inhibitor, inhibiting HDAC1, HDAC2, HDAC3, and HDAC6 with IC50s of 0.7 nM, 1.0 nM, 2.0 nM, and 9.3 nM, respectively.Crebinostat increases the density of synapsin-1 punctae along dendrites in neurons in vitro. Crebinostat increased the density of synapsin-1 punctae along dendrites in neurons in vitro. crebinostat modulated chromatin-mediated neuroplasticity and enhanced memory in mice. crebinostat induced histone H3 and histone H4 acetylation and enhanced the expression of the cAMP-responsive element binding protein (CREB) target gene, Egr1. Crebinostat induces histone H3 and histone H4 acetylation and enhances the expression of Egr1, a cAMP response element binding protein (CREB) target. |
靶点活性 | HDAC1:0.7 nM, HDAC2:1.0 nM, HDAC3:2.0 nM, HDAC6:9.3 nM |
体外活性 | Crebinostat (1 μM; 24 h) induces acetylation of AcH4K12 and AcH3K9 in mouse primary neuronal cells with EC50 values of 0.29 μM and 0.18 μM, respectively. It also downregulates Mapt mRNA expression and upregulates Hspa1b (Hsp70) and Bdnf mRNA expression in mouse primary cultured neurons, while increasing histone acetylation and synapsin I punctae along dendrites in primary cultured neurons.[1] |
体内活性 | Crebinostat (25 mg/kg; i.p.; for 10 days; Male C57BL/6J mice) boosts memory in mice during contextual fear conditioning and leads to a rise in overall hippocampal acetylation of H4K12 and H3K9.[1] |
分子量 | 353.41 |
分子式 | C20H23N3O3 |
CAS No. | 1092061-61-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Crebinostat 1092061-61-4 Chromatin/Epigenetic DNA Damage/DNA Repair Epigenetic Reader Domain Histone Acetyltransferase HDAC Inhibitor inhibitor inhibit