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BI-D1870

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产品编号 T6171Cas号 501437-28-1

BI-D1870是一种高度特异性的、可透过血脑屏障的以及RSK的N端AGC激酶结构域的ATP竞争性抑制剂,抑制 RSK1、RSK2、RSK3和 RSK4 的 IC50值分别为 31 nM、24 nM、18 nM 和15 nM。

BI-D1870
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BI-D1870

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纯度: 99.43%
产品编号 T6171Cas号 501437-28-1

BI-D1870是一种高度特异性的、可透过血脑屏障的以及RSK的N端AGC激酶结构域的ATP竞争性抑制剂,抑制 RSK1、RSK2、RSK3和 RSK4 的 IC50值分别为 31 nM、24 nM、18 nM 和15 nM。

规格价格库存数量
1 mg¥ 389现货
2 mg¥ 563现货
5 mg¥ 955现货
10 mg¥ 1,530现货
25 mg¥ 2,520现货
50 mg¥ 3,990现货
100 mg¥ 5,430现货
500 mg¥ 11,300现货
1 mL x 10 mM (in DMSO)¥ 822现货
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产品介绍

生物活性
产品描述
BI-D1870 is a highly specific, blood-brain-permeable, and ATP-competitive inhibitor of the N-terminal AGC kinase domain of RSK, with IC50 values ​​of 31 nM, 24 nM, 18 nM, and 15 nM for RSK1, RSK2, RSK3, and RSK4.
靶点活性
RSK3:18 nM (cell free), RSK2:24 nM (cell free), RSK1:31 nM (cell free), RSK4:15 nM (cell free)
体外活性
方法:将HEK-293细胞与 BI-D1870(10 μM,15分钟,总共4小时) 孵育为了检验BI-D1870是否能抑制细胞中的RSK活性,研究BI-D1870对HEK-293细胞中RSK催化其已知底物磷酸化的影响,使用PMA作为激动剂激活ERK1/ERK2和RSK亚型。
结果:用 BI-D1870 孵育细胞可极大地抑制 PMA 诱导的 GSK3α 和 GSK3β 磷酸化 ,相比之下,BI-D1870在任何时间点对PMA诱导的ERK1/ERK2激活(由Raf和MKK1催化)或CREB在Ser位点的磷酸化几乎没有影响。[1]
方法:BI-D1870(1,2,3,4,5.28或者48小时) 处理口腔癌细胞系 (SCC2095、SCC4、SCC9、Ca922 和 HSC-3) 和NHOK细胞,MTT检测这些细胞的生长情况。
结果: BI-D1870 对 OSCC 细胞表现出剂量反应性抗增殖作用。[3]
方法:用 BI-D1870 (0.5,2μM)处理转染免疫荧光 GFP-LC3 的细胞 48 小时,并在共聚焦显微镜下观察;使用 DAPI 染色定位细胞核,用 BI-D1870 处理 48 小时的观察细胞中 LC3B 的蛋白质印迹。
结果:BI-D1870 诱导自噬,LC3B-II 的蛋白质印迹表明这种诱导具有剂量依赖性。[3]
体内活性
方法:在用 MOG 肽免疫小鼠两天后,BI-D1870(0.5 mg/kg) 腹腔注射到小鼠体内,每隔一天重复注射一次,持续 11 天。
结果:小鼠表现出延迟神经缺陷;BI-D1870 治疗对体重减轻有中等程度的保护作用。[4]
激酶实验
Purified His6–RSK1, His6–RSK2 or GST–RSK21–389:S381E (1–2 units/ml) were assayed for 10 min at 30 °C in a 50 μl assay mixture in Buffer A containing 30 μM substrate peptide (KEAKEKRQEQIAKRRRLSSLRASTSKSGGSQK), 10 mM magnesium acetate and 100 μM of [γ-32P]ATP. Reactions were terminated and analyzed as described previously. The amount of enzyme that catalyzed the phosphorylation of 1 nmol of substrate peptide in 1 min was termed one unit. In order to assay RSK and MSK1 in HEK-293 or Rat-2 cell lysates, these kinases were immunoprecipitated from the cell lysates (0.1 mg of lysate protein for RSK and 0.3 mg for MSK1) and assayed as described previously, except that for RSK assays the immunoprecipitates were washed twice with Buffer A containing 1 mM ATP and twice with Buffer A prior to the assay, as a precaution to ensure dissociation of BI-D1870 from the RSK isoforms [1].
细胞实验
The rat embryo fibroblast cell line, Rat-2 cells were cultured on 10 cm-diameter dishes in Dulbecco's Modified Eagle's medium supplemented with 10% (v/v) FBS. HEK-293 cells were cultured on 10 cm-diameter dishes in Dulbecco's Modified Eagle's medium supplemented with 10% FBS and 1×antimycotic/antibiotic solution. Prior to stimulation, cells were cultured in the absence of serum for 16 h. Inhibitors were dissolved in DMSO at a 1000-fold higher concentration than they were used at. These inhibitors, or the equivalent volume of DMSO as a control, were added to the tissue culture medium 30 min prior to stimulation unless indicated otherwise. The final concentration of DMSO in the culture medium was 0.1% and had no effect on agonist-induced activation or phosphorylation of any of the substrates examined. The cells were stimulated with the indicated agonists and lysed in 1 ml of ice-cold Lysis Buffer and centrifuged at 16000 g at 4 °C for 5 min. The supernatants were frozen in liquid nitrogen and stored at ?80 °C until use. Protein concentrations were determined using the Bradford method with BSA as the standard [1].
动物实验
Myelin oligodendrocyte glycoprotein (MOG) peptide 35–55. (MEVGWYRSPFSRVVHLYRNGK) (BEX) was used to induce EAE in C57/BL6J mice. Mice were injecteds.c. with 200 g of MOG peptide in100 L of PBS emulsified in 100 L complete Freund's adjuvant (CFA) that was further supplemented with five mg mL?1 Mycobacterium tuberculosis (H37Ra). In addition, 500 ng pertussis toxin was injected i.p. on days zero and two. The RSK inhibitor (BI-D1870; 0.5 mg kg?1) was injected i.p. into mice two days after immunization with MOG peptide, and injection was repeated every other day for 11 days. Mice that received only dimethyl sulfoxide (DMSO) solution were used as controls. Paralysis was evaluated according to the following scale: zero, no disease; one, tail limpness; two, hind limb weakness; three, hind limb paralysis; four, forelimb weakness; five, quadriplegia; six, death. For histological analysis, CNS samples were fixed with 4% paraformaldehyde and sliced at 4 m, and then hematoxylin & eosin (H & E) staining was performed [4].
化学信息
分子量391.42
分子式C19H23F2N5O2
CAS No.501437-28-1
SmilesCC(C)CCN1C(C)C(=O)N(C)c2cnc(Nc3cc(F)c(O)c(F)c3)nc12
密度1.297
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 6.88 mg/mL (17.56 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 7.2 mg/mL (18.39 mM), Suspension. Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
溶液配制表
1mg5mg10mg50mg
1 mM2.5548 mL12.7740 mL25.5480 mL127.7400 mL
5 mM0.5110 mL2.5548 mL5.1096 mL25.5480 mL
10 mM0.2555 mL1.2774 mL2.5548 mL12.7740 mL

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments比如您的给药剂量是 10 mg/kg ,每只动物体重 20 g ,给药体积 100 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent DMSO+ 30%PEG300+ 5%Tween 80 + 60% ddH2O. 那么您的工作液浓度为 2 mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
%Tween 80
%ddH2O

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