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NI-57  ≥98%

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包装规格：1mg 5mg 10mg 25mg 50mg in glass bottle
溶解性：溶于DMSO（100mg/mL 超声）
产品描述：基本信息 产品编号：N10663 产品名称：NI-57 CAS: 1883548-89-7   储存条件 粉末 -20℃ 四年     分子式： C19H17N3O4S 溶于液体 -80℃ 六个月 分子量： 383.42 -20℃ 一个月 化学名：      Solubility (25°C)   体外 DMSO 'mg/mL Ethanol   Water   体内（现配现用）     ＜1mg/ml表示微溶或不溶。 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。 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.
保存条件：-20℃

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