Powder: -20°C for 3 years | In solvent: -80°C for 1 year
dBRD9是一种 PROTAC。dBRD9是一种双重作用的分子,一部分连接 Bromodomain-containing protein 9 (BRD9)的溴域,另一部分招募小脑 E3泛素连接酶的配体(ligand that recruits the cereblon E3 ubiquitin ligase)。dBRD9对 MOLM-13细胞中 BRD9具有抑制作用,可使其降解,IC50为104 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 987 | 现货 | ||
2 mg | ¥ 1,530 | 现货 | ||
5 mg | ¥ 2,590 | 现货 | ||
10 mg | ¥ 4,130 | 现货 | ||
25 mg | ¥ 6,870 | 现货 | ||
50 mg | ¥ 9,450 | 现货 | ||
100 mg | ¥ 12,700 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 3,560 | 现货 |
产品描述 | dBRD9 is a PROTAC. dBRD9 is a double-acting molecule, partially containing Bromodomain-containing protein 9 (BRD9), ligand that recruits the cereblon E3 ubiquitin ligase. Ligand that recruits the cereblon E3 ubiquitin ligase. dBRD9 can inhibit the degradation of BRD9 in MOLM-13 cells, and the IC50 is 104 nM. |
靶点活性 | BRD9 (MOLM-13 cells):104 nM |
体外活性 | dBRD9 has prompt rapid BRD9 degradation over a broad range of concentrations. The degraded BRD9 showed significantly enhanced efficacy(10-to-100-fold). These findings reveal the tractability of non-BET bromodomain-containing proteins to chemical degradation and highlight lead compound dBRD9 as a tool for the study of BRD9[1]. |
体内活性 | The final concentration of dBRD9 of 0.3 nM was mixed in silk fibroin hydrogel and injected into mice. It was found that BRD9 degradant alleviated ZOL-related ONJ. The ONJ-dBRD9 group is filled with well-organized newly formed trabecular bone, with 80% reduced incidence rate of osteonecrosis and periosteal reaction compared with the ONJ-control group[1]. |
别名 | dBRD-9, dBRD 9 |
分子量 | 783.83 |
分子式 | C40H45N7O10 |
CAS No. | 2170679-45-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 90.0 mg/mL (114.8 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 | 1.2758 mL | 6.3789 mL | 12.7579 mL | 31.8947 mL |
5 mM | 0.2552 mL | 1.2758 mL | 2.5516 mL | 6.3789 mL | |
10 mM | 0.1276 mL | 0.6379 mL | 1.2758 mL | 3.1895 mL | |
20 mM | 0.0638 mL | 0.3189 mL | 0.6379 mL | 1.5947 mL | |
50 mM | 0.0255 mL | 0.1276 mL | 0.2552 mL | 0.6379 mL | |
100 mM | 0.0128 mL | 0.0638 mL | 0.1276 mL | 0.3189 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。
dBRD9 2170679-45-3 PROTAC PROTACs dBRD-9 dBRD 9 Inhibitor inhibitor inhibit