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PU-WS13  ≥98%

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包装规格：1mg 5mg 10mg in glass bottle
溶解性：溶于DMSO（≥40mg/mL）
产品描述：基本信息 产品编号：P10923 产品名称：PU-WS13 CAS: 1454619-14-7   储存条件 粉末 -20℃ 四年     分子式： C17H20Cl2N6S 溶于液体 -80℃ 六个月 分子量 411.35 -20℃ 一个月 化学名：  8-(3,5-dichlorophenyl)sulfanyl-9-[3-(propan-2-ylamino)propyl]purin-6-amine   Solubility (25°C)   体外 DMSO ≥40mg/mL (97.24mM) 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 2.4310mL 12.1551mL 24.3102mL 5mM 0.4862mL 2.4310mL 4.8620mL 10mM 0.2431mL 1.2155mL 2.4310mL   生物活性 产品描述 一种选择性的 Grp94 抑制剂，EC50 值为 0.22μM。 靶点/IC50 GRP94 0.22μM (EC50) HSP90α 27.3μM (EC50) HSP90β 41.8μM (EC50) TRAP-1 7.3μM (EC50)   体外研究 PU-WS13 is a Grp94 inhibitor, with an EC50 of 0.22μM. PU-WS13 also slightly suppresses Hsp90α, Hsp90β and Trap-1, with EC 50s of 27.3, 41.8 and 7.3μM, respectively. PU-WS13 (2.5-20μM) shows no toxicity on two nonmalignant cell lines. PU-WS13(15μM) disrupts the circular architecture of HER2 at the plasma membrane of SKBr3 cells mediated through Grp94. PU-WS13 inhibits Grp94, and the inhibition induces apoptosis in and reduce the viability of HER2 overexpressing breast cancer cells.   推荐实验方法(仅供参考) 激酶实验： Kinase Assay The Hsp90 FP competition assays are carried out in black 96-well micro-plates in a total volume of 100μL in each well. A stock of 10μM cy3B-GM and PU-FITC3 is prepared in DMSO and diluted with Felts buffer (20mM Hepes (K), pH 7.3, 50mM KCl, 2mM DTT, 5mM MgCl2, 20mM Na2MoO4 and 0.01% NP40 with 0.1mg/mL BGG). To each well is added the fluorescent dye-labeled Hsp90 ligand (6nM cy3B-GM for Hsp90α, Hsp90β and Grp94 and 3nM PU-FITC3 for Trap-1), protein (10nM Hsp90α, 10nM Hsp90β, 10nM Grp94, 30nM Trap-1) and tested inhibitor (including PU-WS13, initial stock in DMSO) in a final volume of 100μL Felts buffer. Compounds are added in duplicate or triplicate wells. For each assay, background wells (buffer only), tracer controls (free, fluorescent dye-labeled Hsp90 ligand only) and bound controls (fluorescent dye-labeled Hsp90 ligand in the presence of protein) are included on each assay plate. The assay plate is incubated on a shaker at 4°C for 24 h, and the FP values (in mP) are measured. The fraction of fluorescent dye-labeled Hsp90 ligand bound to Hsp90 is correlated to the mP value and plotted against values of competitor concentrations. The inhibitor concentration at which 50% of bound fluorescent dye-labeled Hsp90 ligand is displaced is obtained by fitting the data. For cy3B-GM, an excitation filter at 530nm and an emission filter at 580nm are used with a dichroic mirror of 561nm. For PU-FITC3, an excitation filter at 485nm and an emission filter at 530nm are used with a dichroic mirror of 505nm. All of the experimental data are analyzed, and binding affinity values are given as relative binding affinity values (EC50, concentration at which 50% of fluorescent ligand is competed off by compound).   细胞实验:   Cell Assay Cells are treated for 72 h with inhibitors (including PU-WS13) or transfected with Grp94 siRNA or control siRNA, and their viability is assessed using CellTiter-Glo luminescent Cell Viability Assay. The method determines the number of viable cells in culture based on quantification of the ATP present, which signals the presence of metabolically active cells.
保存条件：-20℃

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