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SGC707

SGC707

产品编号 T3084   CAS 1687736-54-4

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。

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SGC707 Chemical Structure
SGC707, CAS 1687736-54-4
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
产品目录号及名称: SGC707 (T3084)
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选择批次  
纯度: 99.75%
纯度: 99.58%
纯度: 98.45%
更多批次查询请联系客服
生物活性
化学信息
存储 & 溶解度
参考文献
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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: 55 mg/mL (184.4 mM)

DMSO: 55 mg/mL (184.4 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

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

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Kaniskan HÜ, et al. Angew Chem Int Ed Engl. 2015 Apr 20;54(17):5166-70.
BAY-598 EZH2-IN-2 Cyproheptadine hydrochloride sesquihydrate MI-3 MS023 trihydrochloride JNJ-64619178 Tanshindiol B EZM0414

相关化合物库

该产品包含在如下化合物库中:
已知活性化合物库 经典已知活性库 细胞重编程化合物库 抑制剂库 染色质修饰分子库 抗衰老化合物库 干细胞分化化合物库 甲基化化合物库 表观遗传库 共价抑制剂库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

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。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% ddH2O
计算 重置

技术支持

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。

Keywords

SGC707 1687736-54-4 Chromatin/Epigenetic Histone Methyltransferase inhibit Inhibitor SGC 707 SGC-707 inhibitor

 

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