Powder: -20°C for 3 years | In solvent: -80°C for 1 year
SGC707 是 PRMT3化学探针,是一种有效的、选择性的、细胞活性的 PRMT3 变构抑制剂,IC50值为 31 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 164 | 现货 | ||
5 mg | ¥ 332 | 现货 | ||
10 mg | ¥ 534 | 现货 | ||
25 mg | ¥ 984 | 现货 | ||
50 mg | ¥ 1,860 | 现货 | ||
100 mg | ¥ 3,160 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 593 | 现货 |
产品描述 | SGC707 is a potent, selective, and cell-active allosteric inhibitor of PRMT3. |
靶点活性 | PRMT3:31 nM, PRMT3:53 nM(Kd) |
体外活性 | In cells, SGC707 binds to PRMT3 and reduces PRMT3-dependent H4R3me2a. SGC707 also stabilizes PRMT3 in both HEK293 and A549 cells with EC50 values of 1.3 μM and 1.6 μM, respectively. [1] |
体内活性 | In CD-1 male mice, SGC707 (30 mg/kg, i.p.) gives good plasma exposure over 6 h with the peak plasma level of 38000 nM, which suggests that SGC707 is suitable for animal studies. [1] |
激酶实验 | PRMT3 biochemical assay: A radioactivity-based assay is optimized and used to determine the inhibition of PRMT3 in vitro. In a scintillation proximity assay (SPA), tritiated S-adenosylmethionine (3H-SAM) served as a methyl donor to methylate biotinylated histone peptide substrate. After completion of the reaction, the reaction mixture is transferred to the wells of a streptavidin / scintillant-coated microplate. The Biotinylated peptides binding to streptavidin coated resin, brings the incorporated 3H-methyl and the scintillant to close proximity. The amount of methylated peptide is quantified by tracing the radioactivity (counts per minute) as measured by the TopCount NXT? Microplate Scintillation and Luminescence Counter. Due to the very acidic nature of the 3H-SAM solution, non-tritiated (cold) SAM is used to supplement the reactions. The C-terminally biotinylated peptide composed of the first 24 amino acids residues of histone H4 (H4 1-24) is used as substrate. The typical assay mixture contained 0.01% Tween-20, 5 mM DTT, 20 nM PRMT3, 0.3 μM B-H4 1-24 and 28 μM (5 μM 3H-SAM plus 23 μM cold SAM) SAM in 20 mM Tris-HCl (pH 7.5) and a final volume of 20 μL. The IC50 values are determined at Km concentrations of both substrates by titration of the compound in the reaction mixture in a range between 2000-0.2 nM. |
细胞实验 | Cells are seeded in 96-well plates and treated with different concentrations of SGC707 for 72 h. Cell viability is determined using Alamar blue 0.01 mg/mL in the media. Resazurin reduction is monitored with 544 nm excitation, measuring fluorescence at 590 nm. (Only for Reference) |
分子量 | 298.34 |
分子式 | C16H18N4O2 |
CAS No. | 1687736-54-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 55 mg/mL (184.4 mM)
DMSO: 55 mg/mL (184.4 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 3.3519 mL | 16.7594 mL | 33.5188 mL | 83.797 mL |
5 mM | 0.6704 mL | 3.3519 mL | 6.7038 mL | 16.7594 mL | |
10 mM | 0.3352 mL | 1.6759 mL | 3.3519 mL | 8.3797 mL | |
20 mM | 0.1676 mL | 0.838 mL | 1.6759 mL | 4.1899 mL | |
50 mM | 0.067 mL | 0.3352 mL | 0.6704 mL | 1.6759 mL | |
100 mM | 0.0335 mL | 0.1676 mL | 0.3352 mL | 0.838 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。
SGC707 1687736-54-4 Chromatin/Epigenetic Histone Methyltransferase inhibit Inhibitor SGC 707 SGC-707 inhibitor