化合物 PP1|T6196|TargetMol

價(jià)格	￥337	￥486	￥786
包裝	1mg	2mg	5mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-09-23

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產(chǎn)品詳情

中文名稱:化合物 PP1	英文名稱:PP1
CAS:172889-26-8	品牌: TargetMol
產(chǎn)地: 美國(guó)	保存條件: Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
純度規(guī)格: 99.97%	產(chǎn)品類別: 抑制劑
貨號(hào): T6196

Product Introduction

Bioactivity

名稱	PP1
描述	PP1 (AGL 1872), a specific and effective Src inhibitor, is with IC50 for Lck/Fyn is 5 nM/ 6 nM, respectively.
細(xì)胞實(shí)驗(yàn)	PP1 is dissolved in DMSO and stored, and then diluted with appropriate medium before use[2]. 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 (anti-leu4, 100 μg/mL). The final volume of the reaction is 115 μL. Reactions are terminated by the addition of 57.5 μL 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[1].
激酶實(shí)驗(yàn)	Protein A-Sepharose beads (prepared as a 50% (w/v) suspension) are added to the antibody/lysate mixture at 250 μL/mL and allowed to incubate for 30 min at 4°C. The beads are then washed twice in 1 mL of lysis buffer and twice in 1 mL of kinase buffer (25 mM HEPES, 3 mM MnCl2, 5 mM MgCl2, and 100 μM 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 (25 μL/well of a 200 μCi/mL solution in kinase buffer). After incubation for 20 min at 20°C, 60 μL of boiling 2× solubilization buffer containing 10 mM 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 50 mM EDTA, 1 mM ATP. Scintillation fluid (100 μL) 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[1].
體外活性	PP1是一種納摩級(jí)別的Lck和FynT抑制劑，能夠抑制T細(xì)胞中抗CD3誘導(dǎo)的蛋白酪氨酸激酶活性（IC50為0.5 μM），對(duì)Lck和FynT具有選擇性，優(yōu)先抑制T細(xì)胞受體依賴的抗CD3誘導(dǎo)T細(xì)胞增殖（IC50為0.5 μM），而對(duì)非T細(xì)胞受體依賴的phorbol 12-myristate 13-acetate/白細(xì)胞介素-2（IL-2）誘導(dǎo)的T細(xì)胞增殖的抑制作用較弱。PP1（1 μM）選擇性抑制IL-2基因的誘導(dǎo)，但不影響粒細(xì)胞-巨噬細(xì)胞集落刺激因子或IL-2受體基因。此外，PP1還能抑制Src（IC50為170 nM）和Hck（IC50為20 nM）。其抑制A-431表皮生長(zhǎng)因子受體自磷酸化的活性較低，為0.25 μM的IC50的50-100倍。PP1還能以IC50約75 nM和1 μM的濃度抑制Kit和Bcr-Abl酪氨酸激酶。PP1能完全阻止M07e細(xì)胞對(duì)SCF的增殖反應(yīng)，IC50為0.5-1 μM。在完整細(xì)胞中，PP1（1 μM）抑制SCF誘導(dǎo)的c-Kit自磷酸化，并阻斷了絲裂原激活蛋白激酶和Akt的激活。PP1抑制在肥大細(xì)胞疾病中發(fā)現(xiàn)的c-Kit的突變活性形式（D814V和D814Y），并在表達(dá)突變c-Kit的大鼠嗜堿性白血病細(xì)胞系RBL-2H3中誘導(dǎo)凋亡。PP1降低FDCP1細(xì)胞中Bcr-Abl的構(gòu)成性激活，并觸發(fā)凋亡，這些FDCP1細(xì)胞表達(dá)信號(hào)轉(zhuǎn)導(dǎo)和轉(zhuǎn)錄激活因子5以及絲裂原活化蛋白激酶。
存儲(chǔ)條件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 4 mg/mL (14.21 mM) Ethanol : < 1 mg/mL (insoluble or slightly soluble)
關(guān)鍵字	PP1 \| AGL1872 \| EI-275 \| AGL-1872 \| PP-1 \| EI275 \| Inhibitor \| PP 1 \| Src \| inhibit \| Apoptosis
相關(guān)產(chǎn)品	Gefitinib \| Metronidazole \| 5-Fluorouracil \| Stavudine \| Tributyrin \| Dextran sulfate sodium salt (MW 4500-5500) \| Myricetin \| Sorafenib \| L-Ascorbic acid \| Acetylcysteine \| Sodium 4-phenylbutyrate \| Kaempferol
相關(guān)庫(kù)	抑制劑庫(kù) \| 經(jīng)典已知活性庫(kù) \| 抗癌化合物庫(kù) \| 已知活性化合物庫(kù) \| 細(xì)胞因子抑制劑庫(kù) \| 激酶抑制劑庫(kù) \| 抗肝癌化合物庫(kù) \| 抗肺癌化合物庫(kù) \| 膜蛋白靶向化合物庫(kù) \| 酪氨酸激酶分子庫(kù)

關(guān)鍵字： EI 275|||AGL 1872|TargetMol

公司簡(jiǎn)介

上海陶術(shù)生物科技有限公司為美國(guó)Target Molecule Corp. ( Target Mol ) 在上海建立的全資子公司。我們與美國(guó)波士頓、德國(guó)慕尼黑的同事一起，為北美、歐洲和亞洲從事藥物研發(fā)和生物學(xué)研究的科學(xué)家提供優(yōu)質(zhì)的產(chǎn)品和專業(yè)的服務(wù)。公司下設(shè)篩選事業(yè)部，化學(xué)事業(yè)部，生物事業(yè)部和新材料部。從虛擬篩選到實(shí)體化合物分子供應(yīng)；從商業(yè)化產(chǎn)品銷售到個(gè)性化定制合成；從對(duì)明確靶點(diǎn)的分子篩選到對(duì)明確分子的多靶點(diǎn)篩選，從高通量篩選到化學(xué)結(jié)構(gòu)優(yōu)化，我們都可以滿足您的科研用品及技術(shù)服務(wù)的需求。經(jīng)過在中國(guó)市場(chǎng)五年的精心耕耘，我們已成為篩選化合物領(lǐng)域優(yōu)秀的供應(yīng)商，為超過五百家學(xué)校和各類企業(yè)提供了品質(zhì)卓越的小分子化合物和藥物篩

成立日期	2013-04-18 （12年）	注冊(cè)資本	566.2651萬人民幣
員工人數(shù)	100-500人	年?duì)I業(yè)額	￥ 1億以上
主營(yíng)行業(yè)	化學(xué)試劑,生物活性小分子	經(jīng)營(yíng)模式	貿(mào)易,試劑,定制,服務(wù)

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公司成立：12年
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