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BDP5290  ≥98%

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包装规格：1mg 5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性：溶于DMSO（12.5mg/mL）
产品描述：基本信息 产品编号： B10792 产品名称： BDP5290 CAS: 1817698-21-7   储存条件 粉末 -20℃ 四年     分子式： C17H18ClN7O 溶于液体 -80℃ 两年 分子量 371.82 -20℃ 一个月 化学名：  4-Chloro-1-(Piperidin-4-Yl)-N-[3-(Pyridin-2-Yl)-1h-Pyrazol-4-Yl]-1h-Pyrazole-3-Carboxamide Solubility (25°C)：   体外:   DMSO 10mg/mL(26.8947mM;Need ultrasonic) 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 2.6895mL 13.4474mL 26.8947mL 5mM 0.5379mL 2.6895mL 5.3789mL 10mM 0.2689mL 1.3447mL 2.6895mL   生物活性 产品描述 BDP5290 is a potent dual inhibitor of ROCK and MRCK with IC50 of 5nM, 50nM, 10nM and 100nM for ROCK1, ROCK2, MRCKαand MRCKβ, respectively. 靶点 ROCK1 ROCK2 MRCKα MRCKβ 5nM (IC50) 50nM (IC50) 10nM (IC50) 100nM (IC50) 体外研究 The Ki of BDP5290 for MRCKα is 10nM, which is slightly more than the Ki of 4 nM for MRCKβ. 3μM BDP5290 completely inhibits myosin II light chain (MLC) phosphorylation induced by MRCKβ, but not by ROCK1 or ROCK2. At higher concentrations, BDP5290 reduces MLC phosphorylation (pMLC) to undetectable levels. BDP5290 reduces MDA-MB-231 invasion at all tested concentrations starting from 0.1μM, with virtually complete inhibition at 10μM. After 24 hours in the presence of BDP5290 cell viability is slightly reduced with an EC50 >10μM. Wound closure is inhibited by >60% at 1μM BDP5290, a concentration that has no effect on cell viability   推荐实验方法(仅供参考) Kinase Assay MRCKα, MRCKβ, ROCK1 and ROCK2 assays are performed using an IMAP fluorescence polarization assay format. 8 to 12nM of each kinase is incubated for 60 min at room temperature with 100 nM FAM-S6-ribosomal protein derived peptide in the presence of 1μM ATP and 0.5mM MgCl2 in 20mM Tris buffer (pH 7.4) containing 0.01% Tween-20 and 1mM DTT (MRCKα and β); or 1μM ATP, 10mM MgCl2 in 20mM Tris buffer (pH 7.5) containing 0.25mM EGTA 0.01% Triton X-100 and 1mM DTT (ROCK1 and ROCK2). Typically, dose response analysis are performed over concentration ranges from 0.005 to 100μM. Reactions are stopped by adding 2 assay volumes of 0.25% (v/v) IMAP binding reagent in 1×IMAP binding buffer. After 30 min incubation to allow binding reagent to bind phosphorylated peptide, fluorescence polarization is measured on a plate reader at excitation (470 nm) and emission (530nm) wavelengths. Inhibition is calculated using no inhibitor and no enzyme controls as 0 and 100% inhibition, respectively. Kinase selectivity profiling is performed by Eurofins with 10μM ATP and 10 μ M BDP5290   Cell Assay MDA MB 231 or SCC12 cells are plated in a 96 well plate and cultured for 24 hours. Cells are then cultured for 24 hours in SCC12 medium with DMSO vehicle or indicated concentrations of BDP5290 in an IncuCyte ZOOM. Pictures are taken every 3 hours and confluence is measured using the IncuCyte analysis software. AlamarBlue is added to the medium and the cells are cultured for an additional day. Absorbances at 570 nm and at 600 nm are measured to assess cell health
保存条件：-20℃

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