Powder: -20°C for 3 years | In solvent: -80°C for 1 year
SGC2085是一种高效选择性CARM1抑制剂,IC50值为50 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 783 | 现货 | ||
2 mg | ¥ 1,150 | 现货 | ||
5 mg | ¥ 2,290 | 现货 | ||
10 mg | ¥ 3,390 | 现货 | ||
25 mg | ¥ 5,460 | 现货 | ||
50 mg | ¥ 7,430 | 现货 | ||
100 mg | ¥ 9,830 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,650 | 现货 |
产品描述 | SGC2085 is an effective and selective coactivator-associated arginine methyltransferase 1 (CARM1) inhibitor (IC50: 50 nM). |
靶点活性 | CARM1:50 nM |
体外活性 | With the exception of PRMT6 (IC50=5.2 μM), SGC2085 does not inhibit other PRMTs. SGC2085 also shows complete selectivity against a panel of 21 human protein methyltrans- ferases tested at three different concentrations (1,10, and 50 μM). To characterize the mechanism of action of SGC2085 in solution, IC50 values are determined at various concentrations of SAM and peptide substrate. Increasing concentration of substrate peptide or cofactor does not affect IC50 values, indicative of a noncompetitive mechanism of inhibition, which has been previously shown for other protein methyltransferase inhibitors binding at the substrate pocket[1]. No cellular activity is observed for SGC2085 when tested up to 10 μM (48 h exposure in HEK293 cells), while methylation of BAF155 is abrogated by 10 μM of the dual CARM1/PRMT6 inhibitor MS049. We assume that the absence of cellular activity for SGC2085 is due to poor permeability[1]. |
细胞实验 | SGC2085 is dissolved in DMSO and diluted with the appropriate medium before use. HEK293 cells are grown in 12-well plates in DMEM supplemented with 10% FBS, penicillin (100 U/mL), and streptomycin (100 μg/mL). Thirty per cent confluent cells are treated with inhibitors or DMSO. After 48 h, media are removed and cells are lysed in 100 μL of total lysis buffer (20 mM Tris-HCl pH 8.0, 150 mM NaCl, 1 mM EDTA, 10 mM MgCl2, 0.5% Triton X-100, 12.5 U/mL benzonase), complete EDTA-free protease inhibitor cocktail. After 3 min incubation at room temperature, SDS is added to 1% final concentration. Lysates are run on SDS-PAGE, and immunoblotting is done as outlined below to determine the levels of unmethylated and methylated BAF155[1]. |
分子量 | 312.41 |
分子式 | C19H24N2O2 |
CAS No. | 1821908-48-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 40 mg/mL
H2O: Insoluble
DMSO: 55 mg/mL (176.05 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.2009 mL | 16.0046 mL | 32.0092 mL | 80.023 mL |
5 mM | 0.6402 mL | 3.2009 mL | 6.4018 mL | 16.0046 mL | |
10 mM | 0.3201 mL | 1.6005 mL | 3.2009 mL | 8.0023 mL | |
20 mM | 0.16 mL | 0.8002 mL | 1.6005 mL | 4.0012 mL | |
50 mM | 0.064 mL | 0.3201 mL | 0.6402 mL | 1.6005 mL | |
100 mM | 0.032 mL | 0.16 mL | 0.3201 mL | 0.8002 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。
SGC2085 1821908-48-8 Chromatin/Epigenetic Histone Methyltransferase Inhibitor inhibit SGC 2085 SGC-2085 inhibitor