| 中文名称: | SGC2085 | ||||
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| 英文名称: | SGC2085 | ||||
| 别名: | (2S)-2-氨基-N-[[4-(3,5-二甲基苯氧基)-3-甲基苯基]甲基]丙酰胺 SGC2085;SGC-2085 | ||||
| CAS No: | 1821908-48-8 | 分子式: | C19H24N2O2 | 分子量: | 312.41 |
| CAS No: | 1821908-48-8 | ||||
| 分子式: | C19H24N2O2 | ||||
| 分子量: | 312.41 | ||||
基本信息
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产品编号：S10794 |
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产品名称：SGC2085 |
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CAS: |
1821908-48-8 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
六个月 |
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分子量： |
312.41 |
-20℃ |
一个月 |
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化学名： |
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Solubility (25°C) |
体外 |
DMSO |
62mg/mL (198.45mM) |
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Ethanol |
62mg/mL (198.45mM) |
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Water |
Insoluble |
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体内（现配现用） |
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＜1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
3.2009mL |
16.0046mL |
32.0092mL |
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5mM |
0.6402mL |
3.2009mL |
6.4018mL |
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10mM |
0.3201mL |
1.6005mL |
3.2009mL |
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50mM |
0.0640mL |
0.3201mL |
0.6402mL |
生物活性
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产品描述 |
一种具有高效性和选择性的CARM1抑制剂,IC50值为50nM。 |
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靶点/IC50 |
CARM1 |
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50nM |
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体外研究 |
SGC2085 which features a methyl at position R1 and a 3,5-dimethylphenoxy at R2 has an IC50 of 50nM for CARM1 and is over 100-fold selective for CARM1 over PRMT6.These results indicate that the presence of a substituent at R1 is essential for potent and selective inhibition of CARM1.With the exception of PRMT6 (IC50=5.2μM),SGC2085 does not inhibit other PRMTs.Considering its small size (MW=312.4 Da),SGC2085 has an excellent selectivity profile,which can probably be further improved by exploiting differences in the binding sites of the two enzymes outside the arginine binding pocket.Compound SGC2085 also shows complete selectivity against a panel of 21 human protein methyltrans- ferases tested at three different concentrations (1,10,and 50μM). 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. No cellular activity is observed for SGC2085 when tested up to 10μM (48h exposure in HEK293 cells),while methylation of BAF155 is abrogated by 10μM of the dual CARM1/PRMT6 inhibitor MS049.We assume that the absence of cellular activity for SGC2085 is due to poor permeability. |
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体内研究 |
除了PRMT6(IC50=5.2μM)，SGC2085不抑制其他PRMTs。尽管CARM1(PRMT4)被报道能够不对称地对BAF155的R1064位二甲基化，但是在浓度高达10μM时，依然没有观察到SGC2085的细胞活性，这可能是由于其细胞通透性较差。 |
推荐实验方法(仅供参考)
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细胞实验: |
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SGC2085 is dissolved in DMSO and diluted with appropriate medium before use.HEK293 cells are grown in 12-well plates in DMEM supplemented with 10% FBS,penicillin (100 U/mL),and streptomycin (100μg/mL).Thirty percent confluent cells are treated with inhibitors or DMSO.After 48h,media are removed and cells are lysed in 100μL of total lysis buffer (20mM TrisHCl pH 8.0,150mM NaCl,1mM EDTA,10mM MgCl2,0.5% Triton X-100,12.5U/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. |
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
