中文名称: | NI-57 | ||||
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英文名称: | NI-57 | ||||
CAS No: | 1883548-89-7 | 分子式: | C19H17N3O4S | 分子量: | 383.42 |
CAS No: | 1883548-89-7 | ||||
分子式: | C19H17N3O4S | ||||
分子量: | 383.42 |
基本信息
产品编号:N10663 |
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产品名称:NI-57 |
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CAS: |
1883548-89-7 |
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: |
383.42 |
-20℃ |
一个月 |
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化学名: |
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Solubility (25°C) |
体外 |
DMSO |
'mg/mL |
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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 |
2.6081mL |
13.0405mL |
26.0811mL |
5mM |
0.5216mL |
2.6081mL |
5.2162mL |
10mM |
0.2608mL |
1.3041mL |
2.6081mL |
生物活性
产品描述 |
一种溴结构域和植物同源锌指结构域 (BRPF) 蛋白家族的抑制剂,对 BRPF1,BRPF2 (BRD1) 和 BRPF3 的 IC50 值分别为 3.1,46 和 140nM。 |
靶点/IC50 |
3.1nM (BRPF1),46nM (BRPF2 (BRD1)),140nM (BRPF3) |
体外研究 |
NI-57 is an inhibitor of bromodomain and plant homeodomain finger-containing (BRPF), with IC50s of 3.1, 46 and 140nM for BRPF1, BRPF2 (BRD1) and BRPF3,respectively. NI-57 binds the BRD of BRPF1 with a Kd of 31 ± 2nM, BRD1 with a Kd of 110±13nM, and BRPF3 with a Kd of 410±47nM, whereas binding to BRD9 is weaker (Kd 1000±130nM) measured by isothermal titration calorimetry.NI-57 shows less active effect on BRD9 (IC50, 520nM) and BRD4 (BD1 (IC50,3700nM), TRIM24 (IC50,1600nM). NI-57 also inhibits BRPF BRDs in the nucleus, but shows little effect on the proliferation of many cancer cell lines with GI50s of 10.4μM (NCI-H1703 cells),14.7μM (DMS114), 15.6μM (HRA-19), and 16.6μM (RERF-LC-Sq1). Furthermore,Inhibition on BRPF1 of NI-57 (10μM) reduces the gene expression of CCL-22 by 27.7 ± 9.4%. |
体内研究 |
NI-57 has favorable oral bioavailability in mice. |
推荐实验方法(仅供参考)
激酶实验: |
All reagents are diluted in the recommended buffer (50mMHEPES, 100mM NaCl, 0.1% BSA;pH=7.4) supplemented with 0.05% CHAPS and allowed to equilibrate to room temperature prior to addition to plates. 4mL of HIS-tagged protein is added to low-volume 384-well plates,followed by 4mL of either buffer, non-biotinylated peptide, solvent or compounds (NI-57,etc.). Plates are sealed and incubated at room temperature for 30 minutes, before the addition of 4mL biotinylated peptide, resealing and incubation for a further 30 minutes. 4mL of streptavidin-coated donor beads (25µg/mL) and 4 µL of nickel chelate acceptor beads (25µg/mL) are then added under low light conditions. Plates are foil sealed to protect from light, incubated at room temperature for 60 minutes and read on a PHERAstar FS plate reader using an AlphaScreenTM 680 excitation/570 emission filter set. IC50s are calculated in GraphPad Prism 5.Results for compounds (NI-57, etc.) dissolved in DMSO are normalised against corresponding DMSO controls prior to IC50 determination, which are given as the final concentration of compound in the 20µL reaction volume. |
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 )