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受注：045-509-1970 |
技術サポート：tech@selleck.co.jp 平日9:00〜18:00 1営業日以内にご連絡を差し上げます |
化学情報
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Synonyms | KY 12420, SL-2052, BRN 0067676, NSC 627609 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
| 化学式 | C23H24O8 |
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| 分子量 | 428.43 | CAS No. | 19545-26-7 | |
| Solubility (25°C)* | 体外 | DMSO | 86 mg/mL (200.73 mM) | |
| Water | Insoluble | |||
| Ethanol | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
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溶剤液（一定の濃度）を調合する
生物活性
| 製品説明 | Wortmannin is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Wortmannin blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays. Wortmannin also inhibits PLK1 activity. |
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| in vitro | The inhibition of MLCK by Wortmannin is not affected by calmodulin or peptide substrat, while reduced by high concentration of ATP. This compound directly interacts with the catalytic domain of MLCK and leads to an irreversible loss of the enzyme activity. It has no inhibitory to cAMP-dependent protein kinase, cGMP-dependent protein kinase, and calmodulin-dependent protein kinase II, and has little effect on protein kinase C activity. [1] This inhibitor inhibits N-formylmethionyl-leucylphenylalanine (fMLP)-stimulated PtdInsP3 (phosphatidylinositol 3,4,5-trisphosphate) formation with IC50 of 5 nM and this inhibition is completely abolished when pretreated with 100 nM of this compound in human neutrophils, with increased PtdInsP2 levels and no effects on cellular PtdInsP and PtdIns contents. It could develop oscillatory changes in F-actin content and does not inhibit fMLP-stimulated actin polymerization in neutrophils. [2] This chemical irreversibly inhibits phosphatidylinositol 3-kinase (PI3-kinase) activity with binding to the 110-kDa protein (IC50 of 3 nM) and has no effect PI4-kinase in RBL-2H3 cells. It also inhibits leukotriene release, with no effect on the activation of the tyrosine kinase Lyn. [3] This compound completely abolishes the induced hexose uptake in isolated rat adipocytes at 0.1 μM, without impairing stimulated lipolytic activity. [4] It suppresses induced production of nitric oxide by 50% at 500 nM in human umbilical vein endothelial cells, which is in response to IGF-1. [5] This chemical suppresses DNA double strand break (DSB) repair and has no effect on DSB levels or the kinetics of single strand break (SSB) repair in Chinese hamster ovary cells at 50 μM. It could potentiate ionizing radiation (IR)-induced cytotoxicity with no toxicity by itself. [6] This inhibitor inhibits polo-like kinase (PLK1) activity IC50 of 24 nM in intact G2/M-arrested cells. [7] It increases Toll-like receptor (TLR)-mediated accumulation of IL-6 in human macrophages with EC50 of 50 nM. Meanwhile this compound significantly enhances TLR-mediated inducible nitric-oxide synthase (iNOS) expression and nitrite accumulation in mouse macrphages. It activates the nuclear factor-κB and up-regulates the cytokine mRNA production. [8] This chemical also inhibits Polo-like kinase (PlK) 1 and PlK3, which play important roles in mitosis. Its treatment could lead to a reduction in phosphorylation of p53 on serine 20 induced by DNA damage. [9] It suppresses hyaluronan-induced Akt phosphorylation and cell motility/migration in SW1990 cells. [10] |
| in vivo | Wortmannin inhibits peritoneal metastasis of SW1990 in mice at 1 mg/kg, without any weight loss. [10] This compound inhibits phosphatidylinositide 3-kinase-protein kinase B (PKB)/Akt phosphorylation in both normal tissues (lung, heart and brain homogenates) and tumor tissue in mice, without mortality or acute toxicity at 0.7 mg/kg. Combination with LY188011, this chemical significantly increases apoptosis and inhibit tumor growth in orthotopic tumor, while both monotherapy could not. [11] |
プロトコル(参考用のみ)
| キナーゼアッセイ | MLCK assay | |
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| MLCK activity is assayed with peptide substrate (KKRPQRATSNVFS-NH2) or myosin light chain. The peptide substrate (24 μM) is phosphorylated in a reaction mixture containing 25 mM Tris-HC1 (pH 7.5), 0.5 mg/mL bovine serum albumin, 4 mM MgCl2, 0.5 mM CaCl2, 2.6 nM calmodulin, 1.5 nM MLCK, and 400 μM ATP in a final volume of 0.25 mL. After a 10-min preincubation at 28 ºC without ATP, the reaction is started by addition of ATP at 28 ºC and terminated by the addition of 0.1 mL of 10% (v/v) acetic acid after 30 min. The mixture is analyzed by high performance liquid chromatography: column, Unisil Pack 5C18 4.6 X 150 mm; solvent, 18% (v/v) acetonitrile, 0.1% (v/v) trifluoroacetic acid in water; flow rate, 1.0 mL/min; temperature, 40 ºC; detection, absorbance at 220 nm. Percent of reaction is calculated from the ratio of peak areas of phosphorylated form to those of unphosphorylated form. Specific activity measured under the conditions described above is 0.81 μmol/min/mg. Myosin light chain (108 μg/mL) is phosphorylated in a reaction mixture containing 25 mM Tris-HC1 (pH 7.5), 0.5 mg/mL bovine serum albumin, 4 mM MgCl2, 0.5 mM CaCl2, 4.2 nM calmodulin, 0.92 nM enzyme, and 10 μM[γ-32P]ATP (100-900 cpm/pmol) in a final volume of 0.25 mL. After a 3-min preincubation at 30 ºC without ATP, the reaction is started by the addition of [γ-32P]ATP at 30 ºC and stopped by the addition of 0.125 mL of trichloroacetic acid after 5 min. The acid-precipitable materials are collected on a nitrocellulose membrane filter and washed with four 1-mL aliquots of 5% (v/v) trichloroacetic acid. The radioactivity on the filter is measured in a toluene scintillation fluid, using a Packard Tri-Carb liquid scintillation spectrometer Model 4530. The specific activity measured under the conditions is 1.23 μmol/min/mg. [1] | ||
| 細胞アッセイ | 細胞株 | NK cells |
| 濃度 | 1 μM | |
| 反応時間 | 1 h | |
| 実験の流れ | Primary NK cells were pretreated with wortmannin (1 μM) for 1 h, washed twice with RPMI 1640, and then treated with IL-15 (10 ng/mL) for 24 h. DMSO was used as control. |
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| 動物実験 | 動物モデル | Human pancreatic adenocarcinoma cells PK1 are injected both s.c. and orthotopically into SCID mice. |
| 投薬量 | 0.175, 0.35, and 0.7 mg/kg | |
| 投与方法 | Injected by i.v. | |
参考
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カスタマーフィードバック
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Data from [Mol Cancer Ther, 2014, 13(1), 37-48]
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, 2014, Dr.Milica Pesic from Institute for Biological Research
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Data from [Int J Mol Sci, 2013, 14(9), 17304-18]
Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：
| USP5 stabilizes YTHDF1 to control cancer immune surveillance through mTORC1-mediated phosphorylation [ Nat Commun, 2025, 16(1):1313] | PubMed: 39900921 |
| Cardiolipin inhibits the non-canonical inflammasome by preventing LPS binding to caspase-4/11 [ EMBO J, 2025, 10.1038/s44318-025-00507-z] | PubMed: 40670771 |
| Selective tubulin-binding drugs induce pericyte phenotype switching and anti-cancer immunity [ EMBO Mol Med, 2025, 10.1038/s44321-025-00222-6] | PubMed: 40140727 |
| Mechanical force-induced oncostatin M secretion by Jun-positive neutrophils promotes craniofacial bone regeneration for midface hypoplasia treatment [ Stem Cell Res Ther, 2025, 16(1):330] | PubMed: 40598376 |
| Siramesine induced cell death of glioblastoma through inactivating the STAT3-MGMT signaling pathway [ J Transl Med, 2025, 23(1):780] | PubMed: 40640878 |
| Depleting the action of EZH2 through PI3K-mTOR inhibition to overcome metastasis and immunotherapy resistance in triple-negative breast cancer [ Mol Cancer Ther, 2025, 10.1158/1535-7163.MCT-24-0693] | PubMed: 40497697 |
| Cepharanthine hydrochloride: a novel ferroptosis-inducing agent for prostate cancer treatment [ Front Pharmacol, 2025, 16:1536375] | PubMed: 40066333 |
| Intracellular Sphingosine-1-Phosphate Induces Lipolysis Through Direct Activation of Protein Kinase C Zeta [ FASEB J, 2025, 39(7):e70528] | PubMed: 40193069 |
| Vegfr3 activation of Pkd2l1+ CSF-cNs triggers the neural stem cell response in spinal cord injury [ Cell Signal, 2025, 130:111675] | PubMed: 39986360 |
| RhFGF21 protected PC12 cells against mitochondrial apoptosis triggered by H2O2 via the AKT-mediated ROS signaling pathway [ Exp Cell Res, 2025, 445(1):114417] | PubMed: 39793749 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。