切换导航

Wortmannin

现货
Catalog No.
A8544
PI3K抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,100.00
现货
5mg
¥ 790.00
现货
10mg
¥ 1,190.00
现货
20mg
¥ 1,890.00
现货

电话: 021-55669583

邮箱: sales@apexbio.cn

全球经销商

Background

Wortmannin is a selective and irreversible inhibitor of phosphatidylinositol-3-kinase with IC50 value of 1.9nM [1].

Wortmannin is a microbial product. It is produced by a fungal strain, Talaromyces wortmannin KY12420 and is screened out as a potent inhibitor of myosin light chain kina (MLCK). Wortmannin inhibits MLCK as directly interacting with the catalytic domain but not the calmodulin or the regulatory domains. It is found to be a non-competitive inhibitor. The IC50 value of wortmannin for MLCK is 1.9μM. Wortmannin inhibits the phosphorylation and contraction of myosin light chain in rat aort. As an inhibitor of MLCK, wortmannin is developed as vasodilators and anti-inflammatory agent [2].

Wortmannin is also found to be an inhibitor of PI3K with IC50 of 1.9nM in antiphosphotyrosine immunoprecipitates from Swiss 3T3 cells. The inhibition mode is noncompetitive with respect to ATP. Wortmannin is a highly selective inhibitor of PI3K. It has no inhibition effect on Ptdlns-4-kinase, protein kinase C, c-src protein tyrosine kinase and phosphoinositide-specific phospholipase C [1].

References:
[1] Powis G, Bonjouklian R, Berggren M M, et al. Wortmannin, a potent and selective inhibitor of phosphatidylinositol-3-kinase. Cancer Research, 1994, 54(9): 2419-2423.
[2] Nakanishi S, Kakita S, Takahashi I, et al. Wortmannin, a microbial product inhibitor of myosin light chain kinase. Journal of Biological Chemistry, 1992, 267(4): 2157-2163.

文献引用

1. Ming K, Yuan W, et al. "PI3KC3-dependent autophagosomes formation pathway is of crucial importance to anti-DHAV activity of Chrysanthemum indicum polysaccharide." Carbohydr Polym. 2019 Mar 15;208:22-31. PMID:30658794
2. Yuan W, Deng D,et al."Hyperresponsiveness to interferon gamma exposure as a response mechanism to anti-PD-1 therapy in microsatellite instability colorectal cancer." Cancer Immunol Immunother. 2018 Nov 7. PMID:30406373
3. Wang H, Liu W, et al. "Inhibitor analysis revealed that clathrin-mediated endocytosis is involed in cellular entry of type III grass carp reovirus." Virol J. 2018 May 24;15(1):92. PMID:29793525
4. Jie Wu, Pingfan Guo, et al. "Glucagon-like peptide-1 affects human umbilical vein endothelial cells in high glucose by the PI3K/Akt/eNOS signaling pathway." Turk J Biochem. 2017 09 11.
5. Caster JM, Yu SK, et al. "Effect of particle size on the biodistribution, toxicity, and efficacy of drug-loaded polymeric nanoparticles in chemoradiotherapy." Nanomedicine. 2017 Mar 11. pii: S1549-9634(17)30044-8. PMID:28300658

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt428.43
Cas No.19545-26-7
FormulaC23H24O8
Solubility≥21.42mg/mL in DMSO
Chemical Name(1S,6bR,9aS,11R,11bR)-1-(methoxymethyl)-9a,11b-dimethyl-3,6,9-trioxo-3,6,6b,7,8,9,9a,10,11,11b-decahydro-1H-furo[4,3,2-de]indeno[4,5-h]isochromen-11-yl acetate
SDFDownload SDF
Canonical SMILESO=C1[C@](C([H])([H])[C@@]2([H])OC(C([H])([H])[H])=O)(C([H])([H])[H])[C@](C([H])([H])C1([H])[H])([H])C(C3=O)=C2[C@]4(C([H])([H])[H])C5=C3OC([H])=C5C(O[C@]4([H])C([H])([H])OC([H])([H])[H])=O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

v-sis NIH 3T3细胞

制备方法

在DMSO中的溶解度大于21.4 mg/mL。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。

反应条件

1.3 μM

实验结果

在PDGF刺激的v-sis NIH 3T3细胞中,Wortmannin几乎完全抑制Ptdlns-3-phosphate形成。然而,在静息细胞中,Wortmannin不影响磷脂的模式。

动物实验 [2]:

动物模型

携带原位人胰腺癌异种移植瘤的免疫缺陷小鼠

给药剂量

0 ~ 0.7 mg/kg;静脉注射;0 ~ 4小时

实验结果

在原位人胰腺癌异种移植瘤中,Wortmannin呈时间和剂量依赖性地抑制PKB/Akt磷酸化。在4小时和0.7 mg/kg剂量下,PKB/Akt磷酸化水平趋于平稳。同时,PKB/Akt磷酸化水平最大降低了约50%。

其它注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

References:

[1]. Powis G, Bonjouklian R, Berggren M M, et al. Wortmannin, a potent and selective inhibitor of phosphatidylinositol-3-kinase. Cancer Research, 1994, 54(9): 2419-2423.

[2]. Ng SS, Tsao MS, Nicklee T, Hedley DW. 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.

生物活性

描述 Wortmannin是PI3K的抑制剂,IC50值为3 nM。
靶点 PI3K DNA-PK ATM MLCK ATR  
IC50 3 nM 16 nM 150 nM 170 nM 1.8 μM  

质量控制

化学结构

Wortmannin

相关生物数据

Wortmannin
In Western blot assay, we test whether Wortmannin and 3-Me could inhibit the effect of autophagy in 3T3 cells. The 1mM of inhibitors can suppress the cell survival of 3T3 cells. Due to the death of cell at the high concentration of Wortmannin and 3-Me, they are not fit to test in Western blot assay. The result has been shown that the low concentration of Wortmannin and 3-Me (1μM) significantly enhanced the P62 and inhibited the level of autophagy in 3T3 cells.
Method:Western blot; Cell Lines:3T3 cell lines; Concentrations:1μM~1mM; Incubation Time:24 h.

相关生物数据

Wortmannin

相关生物数据

Wortmannin

相关生物数据

Wortmannin

相关生物数据

Wortmannin

相关生物数据

Wortmannin

相关生物数据

Wortmannin