Powder: -20°C for 3 years | In solvent: -80°C for 1 year
C646 是一种竞争性组蛋白乙酰转移酶 p300选择性抑制剂,Ki 值为 400 nM,对其他乙酰转移酶作用较小。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 312 | 现货 | ||
5 mg | ¥ 496 | 现货 | ||
10 mg | ¥ 813 | 现货 | ||
25 mg | ¥ 1,630 | 现货 | ||
50 mg | ¥ 3,160 | 现货 | ||
100 mg | ¥ 4,530 | 现货 | ||
500 mg | ¥ 9,450 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 532 | 现货 |
产品描述 | C646, a histone acetyltransferase inhibitor, inhibits p300 (Ki: 400 nM, in a cell-free assay). |
靶点活性 | p300/CBP:400 nM(Ki) |
体外活性 | 在脊髓中,C646可使机械痛和热痛觉过敏衰减,且伴有对COX-2表达的抑制.C646在弱灭绝训练后,立即注入到ILPFC,对恐惧消退记忆的整合有增强作用. |
体内活性 | 在体外,C646(10 μM)可抑制86% p300。在对雄激素敏感的阉割性前列腺癌细胞系中,C646(20 μM)通过干扰AR和NF-kB通路,进而诱导细胞凋亡。C646(25 μM)可使细胞的组蛋白H3和H4乙酰化水平降低,并阻断TSA诱导的乙酰化。在小鼠细胞中,C646抑制全部H3K4me3动态乙酰化,且局部横跨启动子和诱导基因的起始位点,引起对RNA聚合酶II相互作用和这些基因激活的干扰作用。 |
激酶实验 | Radioactive assay: IC50 values for the putative p300 HAT inhibitors are determined using the direct radioactive assay described above. Reactions are performed in 20 mM HEPES (pH 7.9), and contained 5 mM DTT, 80 μM EDTA, 40μg/ml BSA, 100 μM H4-15, and 5 nM p300. Putative inhibitors are added over a range of concentrations, with DMSO concentration kept constant (<5%). Reactions are incubated at 30°C for 10 min, then initiated with addition of a 1:1 mixture of 12C-acetyl-CoA and 14C-acetyl-CoA to 20 mM. After 10 min at 30°C, reactions are quenched with 14% SDS (w/v). All concentrations are screened in duplicate. Gels are run, washed, dried, and exposed to a PhosphorImager plate, and production of Ac-H4-15 quantified to obtain IC50s. |
细胞实验 | Histone acetylation assays in mouse cells. C3H10T1/2 mouse fibroblasts are grown in DMEM with 10% FCS at 37°C with 6% CO2. Confluent cultures are rendered quiescent in DMEM with 0.5% FCS for 18-20 hr prior to treatment. Cells are treated with the following compounds: TSA (10 ng/ml [33 nM]), C646 (25 μM), C37 (25 μM). Antibodies are used at the following concentrations: total H3 (1:10000; ab7834; Abcam); H4K12ac (1:2500; 06-761; Upstate). Rabbit anti-H3K9ac (1:10000) antibodies are generated in-house. Histones are isolated from cells by acid extraction, separated by SDS and acid-urea polyacrylamide gel electrophoresis and analyzed by western blotting.(Only for Reference) |
分子量 | 445.42 |
分子式 | C24H19N3O6 |
CAS No. | 328968-36-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 4.45 mg/mL (10 mM), Sonification is recommended
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.2451 mL | 11.2254 mL | 22.4507 mL | 56.1268 mL |
5 mM | 0.449 mL | 2.2451 mL | 4.4901 mL | 11.2254 mL | |
10 mM | 0.2245 mL | 1.1225 mL | 2.2451 mL | 5.6127 mL |
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。
C646 328968-36-1 Apoptosis Autophagy Chromatin/Epigenetic Epigenetic Reader Domain Histone Acetyltransferase Inhibitor C-646 HATs C 646 HAT inhibit inhibitor