Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DCH36_06 ((5E)-1-(3-chloro-4-methylphenyl)-5-[(2E)-3-(furan-2-yl)prop-2-en-1-ylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione) 是一种选择性p300/CBP 抑制剂,介导 p300/CBP 抑制导致白血病细胞中 H3K18 的低乙酰化,有抗肿瘤活性,对p300和CBP 的IC50分别为 0.6 μM 和 3.2 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 625 | 现货 | ||
5 mg | ¥ 1,470 | 现货 | ||
10 mg | ¥ 2,630 | 现货 | ||
25 mg | ¥ 4,390 | 现货 | ||
50 mg | ¥ 6,260 | 现货 | ||
100 mg | ¥ 8,580 | 现货 | ||
500 mg | ¥ 17,200 | 待询 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,560 | 现货 |
产品描述 | DCH36_06 ((5E)-1-(3-chloro-4-methylphenyl)-5-[(2E)-3-(furan-2-yl)prop-2-en-1-ylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione) as a bona fide is a potent p300/CBP inhibitor |
靶点活性 | CBP:3.2 μM, p300:0.6 μM |
体外活性 | DCH36_06 mediated p300/CBP inhibition leading to hypoacetylation on H3K18 in leukemic cells. The suppression of p300/CBP activity retarded cell proliferation in several leukemic cell lines.In addition, DCH36_06 arrested cell cycle at G1 phase and induced apoptosis via activation of capase3, caspase9 and PARP that elucidated the molecular mechanism of its anti-proliferation activity. In transcriptome analysis, DCH36_06 altered downstream gene expression and apoptotic pathways-related genes verified by real-time PCR[1]. |
体内活性 | DCH36_06 blocked the leukemic xenograft growth in mice supporting its potential for?in vivo?use that underlies the therapeutic potential for p300/CBP inhibitors in clinical translation[1]. |
别名 | (5E)-1-(3-chloro-4-methylphenyl)-5-[(2E)-3-(furan-2-yl)prop-2-en-1-ylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione |
分子量 | 372.83 |
分子式 | C18H13ClN2O3S |
CAS No. | 593273-05-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 120 mg/mL (321.86 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.6822 mL | 13.4109 mL | 26.8219 mL | 67.0547 mL |
5 mM | 0.5364 mL | 2.6822 mL | 5.3644 mL | 13.4109 mL | |
10 mM | 0.2682 mL | 1.3411 mL | 2.6822 mL | 6.7055 mL | |
20 mM | 0.1341 mL | 0.6705 mL | 1.3411 mL | 3.3527 mL | |
50 mM | 0.0536 mL | 0.2682 mL | 0.5364 mL | 1.3411 mL | |
100 mM | 0.0268 mL | 0.1341 mL | 0.2682 mL | 0.6705 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。
DCH36_06 593273-05-3 Apoptosis Chromatin/Epigenetic Epigenetic Reader Domain Histone Acetyltransferase HATs hypoacetylation DCH-36_06 inhibit antiproliferative p300 HAT Inhibitor (5E)-1-(3-chloro-4-methylphenyl)-5-[(2E)-3-(furan-2-yl)prop-2-en-1-ylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione anti-tumor CBP inhibitor