Powder: -20°C for 3 years | In solvent: -80°C for 1 year
JQAD1是一种有效的、选择性的组蛋白乙酰转移酶 EP300降解剂(PROTAC;DC50≤31.6nM);其包含 EP300抑制剂A485,通过连接体连接至脑啡肽E3连接酶配体。JQAD1以蛋白酶体依赖的方式导致神经母细胞瘤细胞系中EP300的降解。JQAD1抑制H3K27ac 和EP300的表达水平并诱导细胞凋亡。JQAD1抑制Kelly 细胞异种移植的NSG 小鼠的肿瘤生长。CRC 和MYCN 基因表达水平在JQAD1治疗的肿瘤中下调。JQAD1在诱导EP300降解的浓度下对共活化剂CBP 没有显著影响。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 987 | 现货 | ||
5 mg | ¥ 2,490 | 现货 | ||
10 mg | ¥ 3,980 | 现货 | ||
25 mg | ¥ 6,360 | 现货 | ||
50 mg | ¥ 8,720 | 现货 | ||
100 mg | ¥ 11,700 | 现货 |
产品描述 | JQAD1 is a potent and selective histone acetyltransferase EP300 degrader (PROTAC®; DC50≤ 31.6 nM); comprises an EP300 inhibitor, A485, joined by a linker to a cereblon E3 ligase ligand. JQAD1 brings about degradation of EP300 in neuroblastoma cell lines in a proteasome-dependent manner. JQAD1 suppresses both H3K27ac and EP300 expression levels and induces apoptosis. JQAD1 suppresses tumors growth in NSG mice xenografted with Kelly cells. CRC and MYCN genes are downregulated in tumors treated with JQAD1. JQAD1 exhibits no significant effect on coactivator CBP at concentrations inducing EP300 degradation. |
体外活性 | JQAD1 (0.5 or 1 μ M; 6-96 h) treatment led to early time-dependent induction of sub-G1 peak, indicating that apoptosis of Kelly and NGP cells. JQAD1 (1 μ M; 12-36 h) induced apoptosis of Kelly NB cell. JQAD1 (0.5 μ M; 24 h) treated cells showed up-regulation of BH3 effectors BIM, BID and PUMA, pro-apoptotic mediator BAX and its inhibitors BCL2 and MCL1. JQAD1 (0.5 and 1 μ M; 24 h) destroy expression of MYCN. JQAD1 (0.5 μ M; 24 h) lead to H3K27ac deletion on chromatin. JQAD1 (1.2 nM-20 μ M; 5 days) has extensive CRBN-dependent anti-tumor activity across cancer cell lines. JQAD1 induced degradation of EP300 in a time-dependent manner, at the earliest 16 hours [1]. |
体内活性 | JQAD1 (40 mg/kg; i.p.; once a day, for 21 days) inhibits the tumor growth in NSG mice transplanted with Kelly NB cells [1]. |
分子量 | 932.95 |
分子式 | C48H52F4N6O9 |
CAS No. | 2417097-18-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 90.0 mg/mL (96.5 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 | 1.0719 mL | 5.3593 mL | 10.7187 mL | 26.7967 mL |
5 mM | 0.2144 mL | 1.0719 mL | 2.1437 mL | 5.3593 mL | |
10 mM | 0.1072 mL | 0.5359 mL | 1.0719 mL | 2.6797 mL | |
20 mM | 0.0536 mL | 0.268 mL | 0.5359 mL | 1.3398 mL | |
50 mM | 0.0214 mL | 0.1072 mL | 0.2144 mL | 0.5359 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。
JQAD1 2417097-18-6 Chromatin/Epigenetic Epigenetic Reader Domain JQAD-1 JQAD 1 Inhibitor inhibitor inhibit