ホームページ PI3K/Akt/mTOR PI3K inhibitor - ATM/ATR inhibitor - Autophagy inhibitor - DNA-PK inhibitor - Autophagy inhibitor - PLK inhibitor Wortmannin For research use only.

Wortmannin

別名：KY 12420, SL-2052, BRN 0067676, NSC 627609

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.

Wortmannin化学構造

CAS No. 19545-26-7

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 29500 国内在庫あり
JPY 22000 国内在庫あり
JPY 55500 国内在庫あり

代表番号: 045-509-1970|電子メール：[email protected]
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製品安全説明書

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Wortmannin関連製品

シグナル伝達経路

PI3K Signaling Pathways

PI3Kシグナル伝達経路

PI3K阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
MDA-MB-231 Function assay 1 to 10 uM 24 hrs Inhibition of PI3K in human MDA-MB-231 cells assessed as inhibition of AKT phosphorylation at 1 to 10 uM after 24 hrs by Western blot analysis 24828286
A549 Antiproliferative assay 48 hrs Antiproliferative activity against human A549 cells after 48 hrs by SRB method, IC50 = 11.4 μM. 18630894
A549 Function assay Inhibition of Plk3 in human A549 cells assessed as casein substrate phosphorylation by Western blot, IC50 = 0.22 μM. 17135248
HeLa Function assay Binding affinity for Phosphatidylinositol 3-kinase isolated from HeLa cells; Range is 20-120, Ki = 0.12 μM. 15658870
HeLa Function assay Binding affinity for DNA dependent protein kinase isolated from HeLa cells; Range is 20-120, Ki = 0.12 μM. 15658870
HeLa Function assay Inhibition of AX-7503 binding to recombinant Plk3 expressed in HeLa cells by Western blot, IC50 = 0.049 μM. 17135248
Sf9 Function assay Inhibition of human PI3Kalpha expressed in Sf9 cells by fluorescent polarization assay, IC50 = 0.012 μM. 21121631
M059J Function Assay 12.5 mM 0.5 h abolishes the Ser473/Thr308 phosphorylation of AktPKB  16227394
AT5BIVA Function Assay 12.5 mM 0.5 h abolishes the Ser473/Thr308 phosphorylation of AktPKB  16227394
MRC5VI Function Assay 12.5 mM 0.5 h abolishes the Ser473/Thr308 phosphorylation of AktPKB  16227394
HeLa Function Assay 100 nM  1 h alters the morphology of the transferrin recycling compartment 16890915
SMMC-7721 Apoptosis Assay 200 nM 24 h increases CHX-induced apoptosis 17557191
MHG-U1 Growth Inhibition Assay 10 μM 24 h decreases the proportion of G2/M cells 18787832
RT112  Growth Inhibition Assay 10 μM 24 h decreases the proportion of G2/M cells 18787832
SW1990 Function Assay 0.01-1 μM 1 h inhibits HA-induced Akt phosphorylation 19469020
Namalwa Apoptosis Assay 0.25-1.25 μM 24/48 h induces cell apoptosis in both time- and dose- dependent manner 19757185
Jurkat Apoptosis Assay 0.25-1.25 μM 24/48 h induces cell apoptosis in both time- and dose- dependent manner 19757185
Namalwa Growth Inhibition Assay 0.25-1.25 μM 24/48 h inhibits cell proliferation in both time- and dose- dependent manner 19757185
Mel-HO-TS Apoptosis Assay 4/8 μM 24 h enhances TRAIL-induced apoptosis  24113173
A459 Growth Inhibition Assay 2.5 μM 1-4 d enhances cell growth inhibition treatment with 25490383
H1703 Growth Inhibition Assay 2.5 μM 1-4 d enhances cell growth inhibition treatment with 25490383
HUVECs Cytotoxicity Assay 100 nM 24 h attenuates the abrogative effects of calycosin on VRI-induced cytotoxicity 25450186
MDA-MB-231 Apoptosis Assay 1 μM  48 h decreases the cell survival treated with 25 μM of F1 or F2   25300932
MCF7 Function Assay 100 nM 24 h eliminates E2-induced ARE-Luc activity 25172557
MO59K  Cytotoxicity Assay 5 μM 7 d enhances the cytotoxicity of or 24953561
MO59J Cytotoxicity Assay 5 μM 7 d enhances the cytotoxicity of or 24953561
MO59K  Apoptosis Assay 10 μM 24 h increases the DSB level induced by or 24953561
MO59J Apoptosis Assay 10 μM 24 h increases the DSB level induced by or 24953561
HepG2 Function Assay 100 nM 0.5 h blocks MA-induced Akt phosphorylation 24863350
A549  Growth Inhibition Assay 3 µM  2 h suppresses Akt and GSK3β activation, S-phase arrest, cell apoptosis and caspase-3 activation 24847863
A549  Function Assay 10 μm  16 h modulates the IAV replication and causes retention of NP in the nucleus. 24802111
H520 Function Assay 10 μM 1 h decreases cellular phospho-AKT protein levels 24447935
H1975 Function Assay 10 μM 1 h decreases cellular phospho-AKT protein levels 24447935
MG-63 Apoptosis Assay 10 µM 12 h enhances DP-induced apoptosis 24358301
5637 Apoptosis Assay 10 μM 40 min reverses p21WAF1 expression, CDK expression, and cell inhibition induced by fucoidan 24333868
HEK-293 Function Assay 150nM 16 h decreases CRT activity 24324366
BEL/FU Function Assay 1 mM 24 h decreases protein levels of the PI3K/Akt pathway 24232099
A-375 Apoptosis Assay 4/8 μM 24 h enhances TRAIL-induced apoptosis  24113173
Huh7  Function Assay 3 μM 1 h reduces the virus entry into the cells 24184196
A-375-TS  Apoptosis Assay 4/8 μM 24 h enhances TRAIL-induced apoptosis  24113173
GM00637 Function assay 1 uM Inhibition of recombinant Plk3 expressed in human GM00637 cells at 1 uM assessed as decrease in p53 serine-20 phosphorylation 17135248
Jurkat  Kinase Assay IC50 of 24 nM 15664519
N2a Apoptosis Assay 0.1-10 μM 2 h induces decreased cell viability in a concentration-dependent manner 15842767
HeLa Function Assay 12.5 mM 0.5 h abolishes the Ser473/Thr308 phosphorylation of AktPKB  16227394
SMMC-7721 Function Assay 200 nM 24 h up-regulates β1,4GT1 expression 17557191
K562 Growth Inhibition Assay 24 h IC50=25±0.14 nM 19662361
Jurkat Growth Inhibition Assay 0.25-1.25 μM 24/48 h inhibits cell proliferation in both time- and dose- dependent manner 19757185
MDA-MB-231 Function Assay 400 nM 4 h decreases MMP-9 and IL-8 protein in a dose-dependent manner 22906259
MDA-MB-231 Function Assay 0–400 nM 4 h suppresses Akt phosphorylation in a dose-dependent manner 22906259
Mel-2a Apoptosis Assay 4/8 μM 24 h enhances TRAIL-induced apoptosis  24113173
MeWo Apoptosis Assay 4/8 μM 24 h enhances TRAIL-induced apoptosis  24113173
APRE-19 Apoptosis Assay 5 μM 24 h abolishes FLZ-mediated pro-survival/anti-apoptosis activity 25329617
HT-29  Growth Inhibition Assay 1.5 µM 96 h decreases cell growth which can be inhibited by KYNA 25012123
SK-N-LO Function Assay 100 nM 0.5 h decreases the stimulant effects of on Akt phosphorylation 24654606
HL-60 Function Assay 0.1 μM 72 h blocks cell differentiation 24607273
HepG2  Function Assay 200 nM 0.5 h attenuates FoxO phosphorylation 24535192
SW480  Function Assay 150nM 20 h reduces cellular accumulation of β-catenin 24324366
HepG2 Function Assay 100 nM 24 h attenuates the colonies of the tumor cells with upregulation of Akt1 24297510
HCT 116  Function Assay 100 nM 24 h attenuates the colonies of the tumor cells with upregulation of Akt1 24297510
Mel-HO Apoptosis Assay 4/8 μM 24 h enhances TRAIL-induced apoptosis  24113173
HeLa Function assay 100 nM 10 mins Inhibition of PI3K in human HeLa cells assessed as reduction in EGF-stimulated AKT phosphorylation at S473 at 100 nM preincubated for 10 mins followed by EGF stimulation measured after 5 mins by Western blot analysis 30380865
HeLa Function assay 100 nM 10 mins Inhibition of PI3K in human HeLa cells assessed as reduction in EGF-stimulated AKT phosphorylation at T308 at 100 nM preincubated for 10 mins followed by EGF stimulation measured after 5 mins by Western blot analysis 30380865
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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.
Targets
PI3K [3]
(Cell-free assay)		 DNA-PK [12]
(Cell-free assay)		 ATM [12]
(Cell-free assay)		 MLCK [1]
(Cell-free assay)
3 nM 16 nM 150 nM 170 nM
In Vitro
In vitro

The inhibition of MLCK by Wortmannin is not affected by calmodulin or peptide substrat, while reduced by high concentration of ATP. Wortmannin directly interacts with the catalytic domain of MLCK and leads to an irreversible loss of the enzyme activity. Wortmannin 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]

Wortmannin 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 Wortmannin in human neutrophils, with increased PtdInsP2 levels and no effects on cellular PtdInsP and PtdIns contents. Wortmannin could develop oscillatory changes in F-actin content and does not inhibit fMLP-stimulated actin polymerization in neutrophils. [2]

Wortmannin 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. Wortmannin also inhibits leukotriene release, with no effect on the activation of the tyrosine kinase Lyn. [3]

Wortmannin completely abolishes the induced hexose uptake in isolated rat adipocytes at 0.1 μM, without impairing stimulated lipolytic activity. [4]

Wortmannin 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]

Wortmannin 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. Wortmannin could potentiate ionizing radiation (IR)-induced cytotoxicity with no toxicity by itself. [6]

Wortmannin inhibits polo-like kinase (PLK1) activity IC50 of 24 nM in intact G2/M-arrested cells. [7]

Wortmannin increases Toll-like receptor (TLR)-mediated accumulation of IL-6 in human macrophages with EC50 of 50 nM. Meanwhile Wortmannin significantly enhances TLR-mediated inducible nitric-oxide synthase (iNOS) expression and nitrite accumulation in mouse macrphages. Wortmannin activates the nuclear factor-κB and up-regulates the cytokine mRNA production. [8]

Wortmannin also inhibits Polo-like kinase (PlK) 1 and PlK3, which play important roles in mitosis. Wortmannin treatment could lead to a reduction in phosphorylation of p53 on serine 20 induced by DNA damage. [9]

Wortmannin suppresses hyaluronan-induced Akt phosphorylation and cell motility/migration in SW1990 cells. [10]
Kinase Assay MLCK assay
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]
細胞実験 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.
実験結果図 Methods Biomarkers 結果図 PMID
Western blot p-AKT / AKT / p-GSK3β / GSK3β / Bcl-xl / Bax / Caspase-3 / Cleaved caspase-3 25344912
Immunofluorescence DNMT1 24001151
Growth inhibition assay Cell viability 25344912
In Vivo
In Vivo

Wortmannin inhibits peritoneal metastasis of SW1990 in mice at 1 mg/kg, without any weight loss. [10]

Wortmannin 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, Wortmannin significantly increases apoptosis and inhibit tumor growth in orthotopic tumor, while both monotherapy could not. [11]
動物実験 動物モデル Human pancreatic adenocarcinoma cells PK1 are injected both s.c. and orthotopically into SCID mice.
投与量 0.175, 0.35, and 0.7 mg/kg
投与経路 Injected by i.v.

化学情報

分子量 428.43 化学式

C23H24O8
CAS No. 19545-26-7 SDF Download Wortmannin SDFをダウンロードする
Smiles CC(=O)OC1CC2(C(CCC2=O)C3=C1C4(C(OC(=O)C5=COC(=C54)C3=O)COC)C)C
保管

In vitro
Batch:

DMSO : 85 mg/mL ( (198.39 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

mg/kg g μL 匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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