首页Chromatin/EpigeneticEpigenetic Reader DomainC646
C646
编号 T2452    
CAS 328968-36-1     分子式 C24H19N3O6     分子量 445.42
靶点: p300/CBP;
C646, a histone acetyltransferase inhibitor, inhibits p300 (Ki: 400 nM, in a cell-free assay).
纯度:99.0%
规格 库存 单价 数量
2 mg 上海现货 296.00
5 mg 上海现货 532.00
10 mg 上海现货 889.00
25 mg 上海现货 1998.00
50 mg 上海现货 3298.00
100 mg 上海现货 5936.00
1 mL * 10 mM (in DMSO) 上海现货 532.00
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生物活性

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,400nM(Ki)

实验溶液

1% DMSO+30% polyethylene glycol+1% Tween 80: 30 mg/mL

体外活性

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(20μM)通过干扰AR和NF-kB通路,进而诱导细胞凋亡。C646(25μM)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。

体内活性

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。

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, 80μM EDTA, 40μg/ml BSA, 100μM 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)

细胞系: C3H10T1/2

动物实验

动物模型:mouse

化学信息

分子量

445.42

分子式

C24H19N3O6

CAS

328968-36-1

溶解度

DMSO: 11.1 mg/mL (25 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

储存条件

store at -80°C

备注

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

配制溶液

1 mg 5 mg 10 mg
1 mM 2.245 ml 11.225 ml 22.451 ml
5 mM 0.449 ml 2.245 ml 4.49 ml
10 mM 0.225 ml 1.123 ml 2.245 ml
50 mM 0.045 ml 0.225 ml 0.449 ml
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本产品收录于以下化合物库中:
  • 经典已知活性库
  • 抗癌化合物库
  • 表观遗传库
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