中文名称: | FMK 9a | ||||
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英文名称: | FMK 9a | ||||
别名: | FMK-9a;FMK9a FMK 9a | ||||
CAS No: | 1955550-51-2 | 分子式: | C23H21FN2O3 | 分子量: | 392.42 |
CAS No: | 1955550-51-2 | ||||
分子式: | C23H21FN2O3 | ||||
分子量: | 392.42 |
基本信息
产品编号:F10298 |
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产品名称:FMK 9a |
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CAS: |
1955550-51-2 |
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 |
392.42 |
-20℃ |
一个月 |
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化学名: |
N-[(1S)-1-Benzyl-2-[(3-fluoro-2-oxo-propyl)amino]-2-oxo-ethyl]naphthalene-1-carboxamide |
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Solubility (25°C) |
体外 |
DMSO |
100mg/mL (254.83mM;Need ultrasonic) |
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Ethanol |
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Water |
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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。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
2.5483mL |
12.7414mL |
25.4829mL |
5mM |
0.5097mL |
2.5483mL |
5.0966mL |
10mM |
0.2548mL |
1.2741mL |
2.5483mL |
生物活性
产品描述 |
一种autophagin-1的抑制剂,在FRET和LRA试验中测定的IC50值分别为80 和73nM。 |
靶点/IC50 |
autophagin-1, FRET assay autophagin-1, LRA assay IC50: 80nM ; 73nM |
体外研究 |
ATG4B or autophagin-1 is a cysteine protease that cleaves ATG8 family proteins. ATG4B plays essential roles in the autophagosome formation and the autophagy pathway. FMK 9a shows strong inhibition of ATG4B, with IC50 values of 80 and 73nM in the TR-FRET and cellular-based LRA assays, respectively. LC−MS/MS study indicates that FMK 9a forms an irreversible covalent bond with the more reactive thiol group of Cys74 located at the catalytic site of ATG4B and thus inactivates ATG4B proteolytic activity. |
体内研究 |
FMK 9a shows moderate solubility (LYSA: 41μg/mL) and high human and mouse liver microsome clearances of 13.9 and 70mL/kg per minute. |
推荐实验方法(仅供参考)
激酶实验: |
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Kinase Assay |
FMK 9a is dissolved in DMSO. 5μL of serial-diluted FMK 9a (1% DMSO) in assay buffer is added into 5μL of purified ATG4B(final 0.1nM) in 384-well plate, and the solution is incubated at room temperature (rt) for 30 min. Then, 5μL of His-GATE-16-GST (final 20nM) is added into the wells, and the solution is incubated for another 30 min. 5μL of detection solution (final 2nM of Eu-anti-His and 20nM of Ulight-anti-GST) is added, and the resulting mixture is incubated at rt for 40 min. |
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 )