Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GSK1379725A 是一种选择性 BPTF 配体,Kd 为 2.8 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 863 | 现货 | ||
5 mg | ¥ 1,980 | 现货 | ||
10 mg | ¥ 3,360 | 现货 | ||
25 mg | ¥ 5,490 | 现货 | ||
50 mg | ¥ 7,680 | 现货 | ||
100 mg | ¥ 9,870 | 现货 | ||
500 mg | ¥ 19,800 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 2,190 | 现货 |
产品描述 | GSK1379725A is a selective BPTF ligand (Kd = 2.8 μM). |
靶点活性 | BPTF:2.8 μM(Kd) |
体外活性 | Although GSK1379725A has been demonstrated to be selective over Brd4, a full selectivity panel against other bromodomains will be needed. A database search using ChEMBL only showed GSK1379725A to be active in five cellular assays (EC50: 500 nM) carried out. Additionally, no kinase activity has been reported for GSK1379725A despite the growing screening use of the PKIS library[1]. From the NMR titration of GSK1379725A, the bound and unbound resonances are separated by 171 Hz, providing an upper bound for the chemical exchange rate. Assuming an association rate of 1×108 M-1 s-1 as a high end for a range of protein-small molecule interactions, (e.g., chymotrypsin: proflavin k1=1.2×108 M-1 s-1), an upper Kd of 8 μM is estimated from this experiment. For a more accurate determination with a non-fluorinated protein, ITC is used as a complementary direct binding assay using unlabeled BPTF. A Kd of 2.8 μM is obtained, consistent with our intermediate exchange resonance broadening by PrOF NMR. |
分子量 | 450.47 |
分子式 | C23H23FN6O3 |
CAS No. | 1802251-00-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (111 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 | 2.2199 mL | 11.0995 mL | 22.199 mL | 55.4976 mL |
5 mM | 0.444 mL | 2.2199 mL | 4.4398 mL | 11.0995 mL | |
10 mM | 0.222 mL | 1.11 mL | 2.2199 mL | 5.5498 mL | |
20 mM | 0.111 mL | 0.555 mL | 1.11 mL | 2.7749 mL | |
50 mM | 0.0444 mL | 0.222 mL | 0.444 mL | 1.11 mL | |
100 mM | 0.0222 mL | 0.111 mL | 0.222 mL | 0.555 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。
GSK1379725A 1802251-00-8 Chromatin/Epigenetic Epigenetic Reader Domain inhibit Inhibitor GSK-1379725A inhibitor