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Wortmannin渥曼青霉素

原价为:¥4769.00。当前价格为:¥4292.00。

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库存 9 件

SKU: MZ0001-50MG 分类: 标签:

描述

Wortmannin渥曼青霉素

 产品标签

Wortmannin 渥曼青霉素;SL-2052;PI3K抑制剂;Polo-like kinase 1 (PLK1) Polo样激酶1抑制剂; MLCK抑制剂;CAS:19545-26-7;

产品信息:

【产品质控:TLCHPLCNMR元素分析】

【产品标准:HPLC纯度各批次都控制在99.5%以上;元素分析控制在99%以上,避免化学合成中的杂质干扰;】

产品名称 产品编号 CAS NO. 规格 价格(元)
Wortmannin (25mM in DMSO) 渥曼青霉素 MZ0001-100UL 19545-26-7 100µl 389
Wortmannin (25mM in DMSO) 渥曼青霉素 MZ0001-500UL 19545-26-7 5×100µl 1089 980
Wortmannin (Powder) 渥曼青霉素 MZ0001-10MG 19545-26-7 10mg 1459 1313
Wortmannin (Powder) 渥曼青霉素 MZ0001-25MG 19545-26-7 25mg 2619 2357
Wortmannin (Powder) 渥曼青霉素 MZ0001-50MG 19545-26-7 50mg 4769 4292

产品描述

渥曼青霉素(Wortmannin),分离自丝状真菌-绳状青霉(Penicillium funiculosum),是一种有效、不可逆且特异的磷脂酰肌醇3-激酶(PI3K)抑制剂(IC50=2~4nM)。具有良好的细胞膜渗透性,与PI3K的催化亚基结合,进而抑制酶的体内外活性。也能阻断自吞噬形成,有效抑制Polo样激酶1(PLK1)(IC50=5.8nM)。

在成纤维细胞中,渥曼青霉素废止PDGF介导的肌醇(3,4,5)P3的生成(IC50=5nM)。在豚鼠中性粒细胞中,抑制fMLP诱导的PIP3和超氧阴离子生成(IC50=50nM),以及磷脂酶D激活。在NGF处理的PC12细胞中,阻断轴突延伸。在大鼠嗜碱粒细胞性白血病细胞(RBL-2H3)中抑制IgE介导的组胺分泌。渥曼青霉素在更高的浓度下能抑制其他激酶,比如肌球蛋白轻链激酶MLCK(IC50=200 nM)和血小板活化因子诱导的MAP激酶活化(IC50=200~300nM)。

我司提供两种形式的渥曼青霉素(Wortmannin),一种以溶于DMSO的储存液形式提供,浓度为25mM,使用更方便;一种以冻干粉的形式提供,更经济实惠;

产品特性

1) CAS NO:19545-26-7

2) 化学名:(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) 同义名:SL-2052, Antibiotic SL-2052, KY 12420, Wartmannin

4) 分子式:C23H24O8

5) 分子量:428.43

6) 纯度:>98%

7) 溶解性(冻干粉):溶于DMSO(50mM),无水乙醇(5mM,温热助溶)

8) 化学结构图:

保存与运输方法

保存:冻干粉置于+ 4℃干燥保存,2年有效;-20℃干燥保存,3年有效;储存液置于-20℃保存,6个月有效;置于-80℃,12个月有效;

运输:冻干粉室温运输;储存液冰袋运输。

注意事项

1) 低温保存的本品需置于室温回温,低速离心至管底后,再开盖使用。对于储存液,在4℃、冰浴等较低温度情况下会凝固而粘在离心管管底、管壁或管盖内,可以25℃水浴温育片刻至全部融解后使用。

2) 本品对人体有毒,操作时请特别小心,并注意有效防护以避免直接接触人体或吸入体内。

3) 本品仅用作科研用途,不得用作临床诊断或治疗,不得用于食品或药品,绝对禁止用在人身上。

4) 为了您的安全和健康,请穿实验服并戴一次性手套操作。

储存液制备

 质量

溶剂体积

浓度

1mg 5mg 10mg

1mM

2.3341 mL 11.6705 mL 23.3410 mL
5mM 0.4668 mL 2.3341 mL

4.6682 mL

10mM 0.2334 mL 1.1671 mL

2.3341 mL

使用方法【源自文献,仅作参考】

文献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

体内研究(动物模型):

动物模型(Animal Model):Tumor-bearing SCID mice (both s.c. and orthotopically implanted with human pancreatic adenocarcinoma cells PK1)

药物配制(Preparation):Wortmannin was dissolved at 0.4 mg/ml in DMSO, and diluted with 0.9% NaCl before use.

实验方法(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.

文献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

体外研究(细胞实验):

动物模型(Animal Model):Hepatocytes from Wistar rats

药物配制(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.

实验方法(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.

结果(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【版权归集奇生物/MKBio懋康所有】

其他信息

重量 50 克
品牌:

懋康MKBio

CAS:

19545-26-7

规格:

50mg

货期:

3