| 中文名称: | PU-WS13 | ||||
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| 英文名称: | PU-WS13 | ||||
| 别名: | 6-氨基-8-[(3,5-二氯苯基)硫基]-N-异丙基-9H-嘌呤-9-丙胺;PU-WS13 抑制剂 8-((3,5-dichlorophenyl)thio)-9-(3-(isopropylamino)propyl)-9H-purin-6-amine | ||||
| CAS No: | 1454619-14-7 | 分子式: | C17H20Cl2N6S | 分子量: | 411.35 |
| CAS No: | 1454619-14-7 | ||||
| 分子式: | C17H20Cl2N6S | ||||
| 分子量: | 411.35 | ||||
基本信息
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产品编号：P10923 |
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产品名称：PU-WS13 |
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CAS: |
1454619-14-7 |
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 |
411.35 |
-20℃ |
一个月 |
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化学名： |
8-(3,5-dichlorophenyl)sulfanyl-9-[3-(propan-2-ylamino)propyl]purin-6-amine |
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Solubility (25°C) |
体外 |
DMSO |
≥40mg/mL (97.24mM) |
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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。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
2.4310mL |
12.1551mL |
24.3102mL |
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5mM |
0.4862mL |
2.4310mL |
4.8620mL |
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10mM |
0.2431mL |
1.2155mL |
2.4310mL |
生物活性
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产品描述 |
一种选择性的 Grp94 抑制剂，EC50 值为 0.22μM。 |
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靶点/IC50 |
GRP94 0.22μM (EC50) |
HSP90α 27.3μM (EC50) |
HSP90β 41.8μM (EC50) |
TRAP-1 7.3μM (EC50) |
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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. |
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推荐实验方法(仅供参考)
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激酶实验： |
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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). |
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细胞实验: |
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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. |
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 )
