中文名称: | PP1 促销 | ||||
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英文名称: | PP1 | ||||
别名: | 蛋白磷酸酯酶-1(抗原) AGL 1872; EI 275 | ||||
CAS No: | 172889-26-8 | 分子式: | C16H19N5 | 分子量: | 281.36 |
CAS No: | 172889-26-8 | ||||
分子式: | C16H19N5 | ||||
分子量: | 281.36 | ||||
MDL: | MFCD01076570 |
基本信息
产品编号:P10805 |
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产品名称:PP1 |
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CAS: |
172889-26-8 |
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 |
281.36 |
-20℃ |
一个月 |
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化学名: |
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Solubility (25°C) |
体外 |
DMSO |
5mg/mL (17.77mM) |
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Ethanol |
Insoluble |
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Water |
Insoluble |
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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。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
3.5542mL |
17.7708mL |
35.5417mL |
5mM |
0.7108mL |
3.5542mL |
7.1083mL |
10mM |
0.3554mL |
1.7771mL |
3.5542mL |
生物活性
产品描述 |
一种有效的选择性 Src 家族抑制剂,抑制 Lck 和 Fyn,IC50 分别为 5 和 6nM。 |
靶点/IC50 |
IC50: 5nM (Lck), 6nM (Fyn), 250 nM (EGFR), >50μM (JAK2 |
体外研究 |
PP1 inhibits Lck (IC50=5nM) and FynT (IC50=6nM) in vitro at concentrations significantly lower than those required to inhibit ZAP-70 (IC50>100μM), JAK2 (IC50>50μM), the EGFR kinase, and protein kinase A. PP1 inhibits whole cell tyrosine phosphorylation and proliferation in T cells stimulated with anti-CD3 and mitogens. PP1 selectively inhibits IL-2 gene expression over GM-CSF and IL-2R gene induction in human T cells. |
推荐实验方法(仅供参考)
激酶实验: |
Protein A-Sepharose beads (prepared as a 50% (w/v) suspension) are added to the antibody/lysate mixture at 250μL/mL and allowed to incubate for 30 min at 4°C. The beads are then washed twice in 1mL of lysis buffer and twice in 1 mL of kinase buffer (25 mM HEPES, 3mM MnCl2, 5mM MgCl2, and 100μM sodium orthovanadate) and resuspended to 50% (w/v) in kinase buffer. Twenty-five microliters of the bead suspension is added to each well of the enolase-coated 96-well high protein binding plate together with an appropriate concentration of compound and [γ-32P]ATP (25μL/well of a 200μCi/mL solution in kinase buffer). After incubation for 20 min at 20°C, 60μL of boiling 2× solubilization buffer containing 10mM ATP is added to the assay wells to terminate the reactions. Thirty microliters of the samples is removed from the wells, boiled for 5 min, and run on a 7.5% SDS-polyacrylamide gel. The gels are subsequently dried and exposed to Kodak X-AR film. For quantitation, films are scanned using a Molecular Dynamics laser scanner, and the optical density of the major substrate band, enolase p46, is determined. Concentrations of compound that causes 50% inhibition of enolase phosphorylation (IC50) are determined from a plot of the density versus concentration of compound. In companion experiments for measuring the activity of compounds against Lck, the assay plate is washed with two wash cycles on a Skatron harvester using 50mM EDTA, 1mM ATP. Scintillation fluid (100μL) is then added to the wells,and P incorporation is measured using a Pharmacia Biotech micro-β-counter. Concentrations of compound that causes 50% inhibition of enzyme activity (IC50) are determined from a plot of the percent inhibition of enzyme activity versus concentration of compound. |
细胞实验: |
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Inhibition of anti-CD3-stimulated tyrosine phosphorylation in purified human peripheral blood T cells is measured as follows. All incubations are carried out at 37°C in an Eppendorf Thermomixer 5436 at a mixing setting of 11. Cells (1×106 in 100 μL of RPMI 1640 medium) are incubated for 15 min with drug prior to a 6-min incubation with 1 μg of anti-CD3/mL (antileu4, 100μg/mL). The final volume of the reaction is 115μL.Reactions are terminated by the addition of 57.5μL of 3×solubilization buffer incubated at 100°C prior to its addition. Samples are mixed, boiled for 5 min, and stored at -70°C. Western blots of these cell lysates, run on 10% SDS-polyacrylamide gels, are probed with a polyclonal anti-phosphotyrosine antibody, and immune complexes are detected with I-labeled protein A (ICN). For quantitation, films are scanned using a Molecular Dynamics laser scanner, and the optical densities of the major substrate band, p70,are quantitated in the presence of anti-CD3 (in the presence and absence of drug).Percent inhibition is calculated as follows: (1-(p70 optical density units in presence of drug/p70 units in absence of drug))×100.IC50 equals the concentration of compound at which 50% inhibition is measured. |
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 )