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Wortmannin

別名: KY 12420, SL-2052, BRN 0067676, NSC 627609 中文名稱：渥曼青霉素

Wortmannin是一種首次命名的PI3K抑制劑，在無細胞試驗中IC50為3 nM，對 PI3K 家族的選擇性較低。Wortmannin 可抑制自噬體的形成，并有效抑制DNA-PK/ATM，在無細胞試驗中IC50為16 nM和150 nM。Wortmannin 也能抑制 PLK1 的活性。

Wortmannin Chemical Structure

Wortmannin Chemical Structure

CAS: 19545-26-7

規(guī)格 價格 庫存 購買數(shù)量
10mM (1mL in DMSO) 1392.31 現(xiàn)貨
5mg 899.84 現(xiàn)貨
20mg 2375.66 現(xiàn)貨
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Wortmannin相關產品

相關信號通路圖

PI3K Signaling Pathways

PI3K信號通路圖

細胞實驗數(shù)據(jù)示例

細胞系 實驗類型 給藥濃度 孵育時間 活性描述 文獻信息
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

產品描述 Wortmannin是一種首次命名的PI3K抑制劑，在無細胞試驗中IC50為3 nM，對 PI3K 家族的選擇性較低。Wortmannin 可抑制自噬體的形成，并有效抑制DNA-PK/ATM，在無細胞試驗中IC50為16 nM和150 nM。Wortmannin 也能抑制 PLK1 的活性。
靶點
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
體外研究(In Vitro)
體外研究活性

鈣或肽底物不影響Wortmannin對MLCK的抑制，但高濃度的ATP會減弱此種抑制。Wortmannin直接與MLCK催化結構域相互作用，導致不可逆轉的酶活性減弱。Wortmannin對cAMP依賴蛋白激酶，cGMP依賴的蛋白激酶，鈣調蛋白依賴激酶II，和蛋白激酶C均無抑制作用。[1]

Wortmannin抑制由fMLP誘導的PtdInsP3（磷脂酰肌醇3,4,5-三磷酸化）形成，IC 50為5 nM 。在人中性粒細胞中，Wortmannin劑量為100 nM時可發(fā)揮完全抑制作用，增加PtdInsP2水平，且對PtdInsP和 PtdIns沒有影響；Wortmannin可動態(tài)調控F-actin水平對fMLP刺激的肌動蛋白聚合無影響。[2]

在RBL-2H3細胞中，Wortmannin通過結合110-kDa蛋白，不可逆的抑制磷酸肌醇3激酶(PI3-kinase)活性（IC 50為3 nM）對，對Pi4-kinase沒有影響。Wortmannin也抑制Fc epsilon RI介導的組胺分泌和白三烯釋放，對酪氨酸激酶Lyn無影響。[3]

在大鼠脂肪細胞中，劑量為0.1 μM的 Wortmannin可完全抑制胰島素誘導的己糖吸收，二不影響異丙腎上腺素刺激的脂肪分解活性。[4]

在人臍靜脈內皮細胞中，在IGF-1的存在下，Wortmannin抑制胰島素誘導一氧化氮生產，IC50為500nM。[5]

在中國倉鼠卵巢細胞中， Wortmannin以50 μM劑量可抑制DNA雙鏈斷裂（DSB）修復，但對DSB水平無影響或單鏈斷裂（SSB）酶活無影響。Wortmannin可加強電離輻射（紅外）誘導的細胞毒作用，但本身無毒性。[6]

Wortmannin抑制水球樣激酶（PLK 1）活性，IC 50為24nM，造成細胞G 2 / M阻滯。[7]

在人巨噬細胞中，Wortmannin增加 Toll樣受體（TLR）介導的白細胞介素- 6的積累，EC 50 = 50 nM。在小鼠巨噬細胞中，Wortmannin顯著增強TLR誘導一氧化氮合酶（iNOS）的表達和亞硝酸鹽積累。Wortmannin激活核因子-κB和上調細胞因子mRNA量。[8]

Wortmannin也抑制水球樣激酶（PlK）1和PlK 3，在有絲分裂中發(fā)揮重要作用。Wortmannin治療可能導致可減少由DNA損傷誘導的p53絲氨酸20位磷酸化。[9]

在SW 1990細胞中，Wortmannin可抑制透明質酸誘導Akt磷酸化和細胞運動/遷移。[10]
實驗圖片 檢測方法 檢測指標 實驗圖片 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
體內研究(In Vivo)
體內研究活性

Wortmannin劑量為1mg/kg可抑移植瘤小鼠中SW1990的腹膜轉移，無重量損失。[10]

Wortmannin抑制在小鼠正常組織（肺，心臟和腦組織勻漿）及腫瘤組織中的phosphatidylinositide 3- B激酶（PKB）/磷酸化Akt，在劑量為0.7 mg/kg時無死亡或急性毒性。與gemcitabine聯(lián)合使用時，可大大增加細胞凋亡和抑制原位腫瘤生長，兩種藥物單獨使用都無以上效果。[11]
動物實驗 Animal Models 人胰腺癌細胞 PK1s.c.和原位注入SCID免疫缺陷小鼠。
Dosages 0.175, 0.35, 和0.7 mg/kg
Administration 靜脈注射

化學信息&溶解度

分子量 428.43 分子式

C23H24O8
CAS號 19545-26-7 SDF Download Wortmannin SDF
Smiles CC(=O)OC1CC2(C(CCC2=O)C3=C1C4(C(OC(=O)C5=COC(=C54)C3=O)COC)C)C
儲存條件(自收到貨起)

體外溶解度
批次：

DMSO : 85 mg/mL ( (198.39 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計算器

體內溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

 動物體內配方計算器

實驗計算

摩爾濃度計算器

質量 濃度 體積 分子量

動物體內配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

mg/kg g μL 只

第二步：請輸入動物體內配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。

體內配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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