Wortmannin
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Wortmannin(渥曼青霉素)是一种选择性的和可逆的磷脂酰肌醇3-激酶抑制剂,IC50值为1.9 nM[1]。
Wortmannin是微生物的产物,由真菌菌株,裸节菌属渥曼青霉素KY12420产生,作为一种有效的肌球蛋白轻链激酶(MLCK)抑制剂而被筛选出来。Wortmannin通过直接与催化结构域,而非钙调蛋白或调节结构域相互作用,从而抑制MLCK。Wortmannin是一种非竞争性的抑制剂,对MLCK的IC50值为1.9 μM。在大鼠主动脉中,wortmannin抑制肌球蛋白轻链的磷酸化和收缩。作为MLCK的抑制剂,wortmannin可用作血管扩张剂和消炎剂[2]。
在Swiss 3T3细胞的抗磷酸酪氨酸免疫沉淀中发现,wortmannin也是PI3K的抑制剂,IC50值为1.9 nM,该抑制模式是ATP非竞争性的。Wortmannin是一种高选择性的PI3K抑制剂,对Ptdlns-4-激酶、蛋白激酶C、c-src蛋白酪氨酸激酶和磷酸肌醇特异性磷脂酶C均无抑制效应[1]。
参考文献:
[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.
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- 3. Xia Li, Yuhan Zhang, et al. "Autophagy Activated by Peroxiredoxin of Entamoeba histolytica." Cells. 2020 Nov 12;9(11):2462. PMID: 33198056
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- 5. 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
- 6. 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
- 7. 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.
- 8. 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
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 428.43 |
Cas No. | 19545-26-7 |
Formula | C23H24O8 |
Solubility | ≥21.42 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH |
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 |
SDF | Download SDF |
Canonical SMILES | O=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 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 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。溶液形式一般不宜长期储存,请尽快用完。 |
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. |
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 |
质量控制和MSDS
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