Powder: -20°C for 3 years | In solvent: -80°C for 1 year
I-BRD9 (GSK602) 是一种选择性的 BRD9 细胞抑制剂,pIC50 为 7.3。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 255 | 现货 | ||
2 mg | ¥ 369 | 现货 | ||
5 mg | ¥ 647 | 现货 | ||
10 mg | ¥ 1,080 | 现货 | ||
25 mg | ¥ 2,160 | 现货 | ||
50 mg | ¥ 3,260 | 现货 | ||
100 mg | ¥ 4,760 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 708 | 现货 |
产品描述 | I-BRD9 (GSK602) is the first selective cellular inhibitor for BRD9 with pIC50 of 7.3. |
靶点活性 | BRD9:7.3 (pIC50) |
体外活性 | I-BRD9 is identified through structure-based design, leading to greater than 700-fold selectivity over the BET family and 200-fold over the highly homologous bromodomain-containing protein 7 (BRD7). I-BRD9 is used to identify genes regulated by BRD9 in Kasumi-1 cells involved in oncology and immune response pathways and to the best of our knowledge, represents the first selective tool compound available to elucidate the cellular phenotype of BRD9 bromodomain inhibition[1]. |
激酶实验 | Receptor binding is performed using membranes prepared from cells with recombinant expression of adenosine receptors as follows: human A2A and HEK 293, rat A2A and Chinese hamster ovary, human and rat A1 and Chinese hamster ovary, and human A3 and HEK 293. Radioligand competition binding assays are performed in 96-well plates in a total assay volume of 200 μL using a final test drug concentration range of between 0.1 and 3 μM. Membranes are diluted in assay buffer, pH 7.4 (A1 and A2A, Dulbecco's phosphate-buffered saline with 10 mM MgCl2; A3, 50 mM Tris-HCl, 120 mM NaCl, 10 mM MgCl2). To remove endogenous adenosine from the membrane preparations, 4 U/mL adenosine deaminase is added to the membranes, which are then incubated at room temperature for 15 min. Radioligand is added to a final concentration of 0.5 ([3H]SCH 58261, A2A), 1 ([3H]DPCPX, A1), or 0.25 ([125I]AB-MECA, A3) nM. Nonspecific binding is defined by adding 100 nM CGS 15923 (A2A), 100 nM NECA (A1), or 100 nM DPCPX (A3). Plates are incubated at room temperature with agitation for 1.5 h (A2A and A1) or 2 h (A3). Membranes are filtered onto Packard GF-B filter plates and washed in ice-cold assay buffer using a Brandel cell harvester to separate bound and free radioligand. The plates are dried before addition of 45 μL of Microscint 20 to each well. |
别名 | GSK602 |
分子量 | 497.55 |
分子式 | C22H22F3N3O3S2 |
CAS No. | 1714146-59-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (100.49 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.0098 mL | 10.0492 mL | 20.0985 mL | 50.2462 mL |
5 mM | 0.402 mL | 2.0098 mL | 4.0197 mL | 10.0492 mL | |
10 mM | 0.201 mL | 1.0049 mL | 2.0098 mL | 5.0246 mL | |
20 mM | 0.1005 mL | 0.5025 mL | 1.0049 mL | 2.5123 mL | |
50 mM | 0.0402 mL | 0.201 mL | 0.402 mL | 1.0049 mL | |
100 mM | 0.0201 mL | 0.1005 mL | 0.201 mL | 0.5025 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。
I-BRD9 1714146-59-4 Chromatin/Epigenetic Epigenetic Reader Domain cancer inhibit bromodomain-containing protein 7(BRD7) bromodomain and extra terminal domain (BET) BRD9 GSK 602 Kasumi-1 cells Inhibitor GSK-602 GSK602 probe I-BRD-9 I BRD9 immune response IBRD9 inhibitor