中文名称: | GSK-J1 | ||||
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英文名称: | GSK-J1 | ||||
别名: | N-[2-(2-吡啶基)-6-(1,2,4,5-四氢-3H-3-苯并氮杂卓-3-基)-4-嘧啶基]-beta-丙氨酸;二溴化钨;N-[2-(2-吡啶基)-6-(1,2,4,5-四氢-3H-3-苯并氮杂卓-3-基)-4-嘧啶基]-BETA-丙氨酸 3-{[2-(pyridin-2-yl)-6-(2,3,4,5-tetrahydro-1H-3-benzazepin-3-yl)pyrimidin-4-yl]amino}propanoic acid | ||||
CAS No: | 1373422-53-7 | 分子式: | C22H23N5O2 | 分子量: | 389.45 |
CAS No: | 1373422-53-7 | ||||
分子式: | C22H23N5O2 | ||||
分子量: | 389.45 |
基本信息
产品编号:G10425 |
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产品名称:GSK-J1 |
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CAS: |
1373422-53-7 |
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: |
389.45 |
-20℃ |
一个月 |
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化学名: |
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Solubility (25°C) |
体外 |
DMSO |
77mg/mL (197.71mM) |
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Ethanol |
Insoluble |
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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。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
2.5677mL |
12.8386mL |
25.6772mL |
5mM |
0.5135mL |
2.5677mL |
5.1354mL |
10mM |
0.2568mL |
1.2839mL |
2.5677mL |
50mM |
0.0514mL |
0.2568mL |
0.5135mL |
生物活性
产品描述 |
一种H3K27me3/me2-demethylases JMJD3/KDM6B 和 UTX/KDM6A 的抑制剂,对 KDM6B 的 IC50 值为 60nM。 |
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靶点/IC50 |
JMJD3 |
UTX |
28nM |
53nM |
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体外研究 |
GSK-J1 is selective for H3K27 demethylases of the KDM6 subfamily and specifically binds to endogenous JMJD3.GSK-J1 inhibits TNF-α production by human primary macrophages in an H3K27-dependent manner.GSK-J1 inhibits the demethylase activity of KDM5C with 8.5-fold increased potency compared with that of KDM5B at 1mM α-ketoglutarate,with IC50 of 11μM and 94μM,respectively. |
推荐实验方法(仅供参考)
激酶实验: |
Purified JmjD3 (1μM) and UTX (3μM) is incubated with 10μM peptide [BiotinKAPRKQLATKAARK(me3 )SAPATGG] in 50mM HEPES pH 7.5,150mM KCl,50μM (NH4)2SO4·FeSO4·H2O,1mM 2-oxoglutarate,and 2mM ascorbate (JmjD3,3 minutes at 25℃;UTX,20 minutes at 25℃) with various concentration of the inhibitor (0,0.005,0.01,0.02,0.05,0.1μM).10mM EDTA is added to stop the reaction.The reaction is desalted by zip tip and spotted on a MALDI plate with α-cyano-4-hydroxycinnamic acid MALDI matrix.Samples are analysed on a MALDI-TOF R system. |
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 )