産品簡介:
Wortmannin渥曼青黴素
産品标簽
Wortmannin 渥曼青黴素;SL-2052;PI3K抑制劑;Polo-like kinase 1 (PLK1) Polo樣激酶1抑制劑; MLCK抑制劑;CAS:19545-26-7;
産品信息:
【産品質控:TLC\HPLC\NMR\元素分析】
【産品标準:HPLC純度各批次都控制在99.5%以上(shàng);元素分析控制在99%以上(shàng),避免化學合成中的雜(zá)質幹擾;】
産品名稱
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産品編号
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CAS NO.
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規格
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價格(元)
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Wortmannin (25mM in DMSO) 渥曼青黴素
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MZ0001-100UL
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19545-26-7
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100µl
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389
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Wortmannin (25mM in DMSO) 渥曼青黴素
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MZ0001-500UL
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19545-26-7
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5×100µl
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1089 980
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Wortmannin (Powder) 渥曼青黴素
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MZ0001-10MG
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19545-26-7
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10mg
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1459 1313
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Wortmannin (Powder) 渥曼青黴素
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MZ0001-25MG
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19545-26-7
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25mg
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2619 2357
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Wortmannin (Powder) 渥曼青黴素
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MZ0001-50MG
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19545-26-7
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50mg
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4769 4292
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産品描述
渥曼青黴素(Wortmannin),分離自(zì)絲狀真菌-繩狀青黴(Penicillium funiculosum),是一(yī)種有效、不可逆且特異的磷脂酰肌醇3-激酶(PI3K)抑制劑(IC50=2~4nM)。具有良好的細胞膜滲透性,與PI3K的催化亞基結合,進而抑制酶的體内外活性。也能(néng)阻斷自(zì)吞噬形成,有效抑制Polo樣激酶1(PLK1)(IC50=5.8nM)。
在成纖維細胞中,渥曼青黴素廢止PDGF介導的肌醇(3,4,5)P3的生(shēng)成(IC50=5nM)。在豚鼠中性粒細胞中,抑制fMLP誘導的PIP3和超氧陰離子生(shēng)成(IC50=50nM),以及磷脂酶D激活。在NGF處理的PC12細胞中,阻斷軸突延伸。在大鼠嗜堿粒細胞性白(bái)血病細胞(RBL-2H3)中抑制IgE介導的組胺分泌。渥曼青黴素在更高(gāo)的濃度下(xià)能(néng)抑制其他激酶,比如肌球蛋白(bái)輕鏈激酶MLCK(IC50=200 nM)和血小(xiǎo)闆活化因子誘導的MAP激酶活化(IC50=200~300nM)。
我司提供兩種形式的渥曼青黴素(Wortmannin),一(yī)種以溶于DMSO的儲存液形式提供,濃度為(wèi)25mM,使用更方便;一(yī)種以凍幹粉的形式提供,更經濟實惠;
産品特性
1) CAS NO:19545-26-7
2) 化學名:(1S,6bR,9aS,11R,11bR)11-(Acetyloxy)-1,6b,7,8,9a,10,11,11b-octahydro-1-(methoxymethyl)-9a,11b- dimethyl-3H-furo[4,3,2-de]indeno[4,5,-h]-2-h]-2-benzopyran-3,6,9-trione
3) 同義名:SL-2052, Antibiotic SL-2052, KY 12420, Wartmannin
4) 分子式:C23H24O8
5) 分子量:428.43
6) 純度:>98%
7) 溶解性(凍幹粉):溶于DMSO(50mM),無水(shuǐ)乙醇(5mM,溫熱助溶)
8) 化學結構圖:
保存與運輸方法
保存:凍幹粉置于+ 4℃幹燥保存,2年(nián)有效;-20℃幹燥保存,3年(nián)有效;儲存液置于-20℃保存,6個(gè)月(yuè)有效;置于-80℃,12個(gè)月(yuè)有效;
運輸:凍幹粉室溫運輸;儲存液冰袋運輸。
注意事(shì)項
1) 低(dī)溫保存的本品需置于室溫回溫,低(dī)速離心至管底後,再開(kāi)蓋使用。對于儲存液,在4℃、冰浴等較低(dī)溫度情況下(xià)會(huì)凝固而粘在離心管管底、管壁或管蓋内,可以25℃水(shuǐ)浴溫育片刻至全部融解後使用。
2) 本品對人體有毒,操作時請特别小(xiǎo)心,并注意有效防護以避免直接接觸人體或吸入體内。
3) 本品僅用作科研用途,不得用作臨床診斷或治療,不得用于食品或藥品,絕對禁止用在人身上(shàng)。
4) 為(wèi)了您的安全和健康,請穿實驗服并戴一(yī)次性手套操作。
儲存液制備
質量
溶劑體積
濃度
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1mg
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5mg
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10mg
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1mM
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2.3341 mL
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11.6705 mL
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23.3410 mL
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5mM
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0.4668 mL
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2.3341 mL
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4.6682 mL
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10mM
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0.2334 mL
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1.1671 mL
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2.3341 mL
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使用方法【源自(zì)文獻,僅作參考】
文獻1,Ng SS et al. Wortmannin inhibits pkb/akt phosphorylation and promotes gemcitabine antitumor activity in orthotopic human pancreatic cancer xenografts in immunodeficient mice. Clin Cancer Res. 2001 Oct;7(10):3269-75. MKBio PMID: 11595724
體内研究(動物(wù)模型):
動物(wù)模型(Animal Model):Tumor-bearing SCID mice (both s.c. and orthotopically implanted with human pancreatic adenocarcinoma cells PK1)
藥物(wù)配制(Preparation):Wortmannin was dissolved at 0.4 mg/ml in DMSO, and diluted with 0.9% NaCl before use.
實驗方法(Assay):A) In the first set of experiments, groups of tumor-bearing SCID mice (n = 4 each) were given single bolus injections of 0.7 mg/kg wortmannin via the tail vein and killed at various time points. B) In a second series of experiments, groups of animals (n = 4 each) were injected i.v. with increasing doses of wortmannin (0.175, 0.35, and 0.7 mg/kg) and killed at 4 h. C) In a third series of experiments, tumor-bearing SCID mice were randomly assigned to four groups (n = 4 each). Each group was given i.v. bolus injections of either the drug vehicle (≤1% DMSO), 80 mg/kg of gemcitabine for 48 h, 0.7 mg/kg of wortmannin for 4 h, or 80 mg/kg of gemcitabine for 48 h and then 0.7 mg/kg wortmannin for 4 h.
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文獻2,Blommaart EF et al. The phosphatidylinositol 3-kinase inhibitors wortmannin and LY294002 inhibit autophagy in isolated rat hepatocytes. MKBio Eur J Biochem. 1997 Jan 15;243(1-2):240-6. PMID: 9030745
體外研究(細胞實驗):
動物(wù)模型(Animal Model):Hepatocytes from Wistar rats
藥物(wù)配制(Preparation):Wortmannin was dissolved in DMSO at 2mM, and stored at -20℃ in the dark. Dilutions in 0.9% NaCl were prepared just before the start of each experiment. The final DMSO concentration in the incubation medium did not exceed 0.25 % (by vol.). This concentration of DMSO did not affect the processes that were tested.
實驗方法(Assay):Electron micrographs of isolated rat hepatocytes that were incubated for 60 min (5 mg dry cells/ml) with 50μM vinblastin alone (A, B) or in the presence of 50μM vinblastin plus 100 nM wortmannin.
結果(Results):Autophagosomes could hardly be detected in cells that were incubated in the presence of 100 nM wortmannin (Fig. 3 C) compared to cells incubated under maximal autophagic conditions (Fig. 3 A and B).
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— —Written/Edited by V. Shallan【版權歸MKBio懋康所有】
上海夢澤生物科技有限公司是一(yī)家涉足于生(shēng)命科學和生(shēng)物(wù)技(jì)術(shù)領域研究的試劑、儀器(qì)和實驗室消耗品與實驗服務工(gōng)作,主要從(cóng)事(shì)細胞生(shēng)物(wù)學、植物(wù)學、分子生(shēng)物(wù)學、免疫學、生(shēng)物(wù)化學、蛋白(bái)組學。生(shēng)物(wù)制藥與診斷試劑研發生(shēng)産等領域。 本公司秉承“以人為(wèi)本,以誠為(wèi)信、合同守信”的經營理念。堅持"品質保障"的原則為(wèi)廣大客戶提供優質産品。
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