中文名称: PP1 促销
英文名称: PP1
CAS No: 172889-26-8
分子式: C16H19N5
分子量: 281.36
P10805 PP1 ≥98% (psaitong)
包装规格:
5mg 25mg 100mg in glass bottle
溶解性:
溶于DMSO(28 mg/mL 超声)
产品描述:

基本信息

产品编号:P10805

产品名称:PP1

CAS:

172889-26-8

 

储存条件

粉末

-20℃

四年

 

 

分子式:

C16H19N5

溶于液体

-80℃

六个月

分子量

281.36

-20℃

一个月

化学名: 

 

 

Solubility (25°C)

 

体外

DMSO

5mg/mL (17.77mM)

Ethanol

Insoluble

Water

Insoluble

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

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:

 

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.

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
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参考文献 & 客户发表文献

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

  • =
    *
    *
    *选择对应的单位 *空出希望得到的变量,填写另外两个变量

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 )

  • * = *

连续稀释计算器方程

  • 连续稀释

  • 初始浓度:
  • 稀释倍数:
  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):